tolvaptan

may enhance the serum concentration when combined with tolvaptan

may enhance the serum concentration when combined with tolvaptan

curcumin

may enhance the serum concentration when combined with tolvaptan

may enhance the serum concentration when combined with tolvaptan

may enhance the serum concentration when combined with tolvaptan

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

citalopram

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

efavirenz

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

primidone

may diminish the serum concentration when combined with tolvaptan

may diminish the serum concentration when combined with tolvaptan

isoniazid

may diminish the serum concentration when combined with tolvaptan

propofol

may diminish the serum concentration when combined with tolvaptan

selexipag

may diminish the serum concentration when combined with tolvaptan

desmopressin

may decrease the therapeutic effect when combined with desmopressin

sodium chloride

may increase the adverse effect when combined with tolvaptan

grapefruit

It may enhance the effect when combined with grapefruit by CYP3A4 metabolism

griseofulvin

It may diminish the effect when combined with griseofulvin by CYP3A4 metabolism

miconazole vaginal

It may enhance the effect when combined with miconazole vaginal by affecting CYP3A4 metabolism

enzalutamide

CYP3A strong enhancers of the small intestine may reduce the bioavailability of tolvaptan

nirmatelvir/ritonavir

may enhance the serum concentration of CYP3A4 inhibitors

sodium chloride nasal

sodium chloride increases the toxicity of tolvaptan

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

losartan

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

may increase the hyperkalemic effect when combined with ace inhibitors

quinapril

may increase the hyperkalemic effect when combined with ace inhibitors

ramipril

may increase the hyperkalemic effect when combined with ace inhibitors

rescinnamine

may increase the hyperkalemic effect when combined with ace inhibitors

spirapril

may increase the hyperkalemic effect when combined with ace inhibitors

may diminish the serum concentration when combined with tolvaptan

efavirenz

may diminish the serum concentration when combined with tolvaptan

digoxin

may enhance the serum concentration when combined with digoxin

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

amiloride

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

dexamethasone

It may enhance the metabolism when combined with dexamethasone

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

losartan

may enhance the hyperkalemic effect

cilazapril

may enhance the hyperkalemic effect

enalapril

may enhance the hyperkalemic effect

enalaprilat

may enhance the hyperkalemic effect

lisinopril

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

amiloride

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

paclitaxel

when both drugs are combined, there may be a high metabolism of tolvaptan 

lorlatinib

the effect of tolvaptan is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism

carvedilol

it enhances the serum potassium levels

telmisartan

it may enhance the serum potassium levels

primidone

may decrease the serum concentration

may decrease the serum concentration

may decrease the serum concentration

efavirenz

may decrease the serum concentration

isoniazid

may decrease the serum concentration

may decrease the serum concentration

donepezil transdermal

may decrease the serum concentration

efavirenz

may decrease the serum concentration

prednisolone

may decrease the serum concentration

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

isoniazid

may increase the serum concentration

mexiletine

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

curcumin

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

diacerein

may increase the serum concentration

may increase the serum concentration

tranylcypromine

may increase the serum concentration

phosphoric acid

the efficacy of phosphoric acid may be decreased due to an increase in rate of excretion

Frequency defined

>10%

Samsca

Pollakiuria (4-11%)
Urinary output increased (11%)
Dry mouth (13%)
Thirst (16%)
Nausea (21%)

Jynarque

Dizziness (11.3%)
Diarrhea (13.3%)
Fatigue (13.6%)
Dry mouth (16%)
Thirst (63.7%)
Increased urination (69.5%)

1-10%

Samsca

Pyrexia (4%)
Anorexia (4%)
Hyperglycemia (6%)
Constipation (7%)
Weakness (9%)
GI bleeding (10%)

Jynarque

Palpitations (3.5%)
Hyperuricemia (3.9%)
Rash (4.2%)
Dry skin (4.9%)
Abdominal distension (4.9%)
Decreased appetite (7.2%)
Dyspepsia (7.9%)

Post marketing Reports

Investigations: Hypernatremia

Hepatobiliary disorders: Liver failure

Neurologic: Osmotic demyelination syndrome

Immune system disorders: anaphylactic shock and rash

Black Box Warning:

tolvaptan has a black box warning, which is the most serious warning issued by the US Food and Drug Administration (FDA). The black box warning for tolvaptan is related to the risk of liver injury and failure.

The warning states that tolvaptan can cause potentially fatal liver injury, including hepatic failure requiring liver transplantation. The risk is highest in patients with underlying liver disease, but it can occur in patients without pre-existing liver disease as well.

Contraindication/Caution:

Contraindication:

Known hypersensitivity: tolvaptan should not be used in patients who have a known hypersensitivity to tolvaptan or any of its components.
Severe liver impairment: tolvaptan is contraindicated in patients with severe liver impairment, such as those with cirrhosis or a Child-Pugh score greater than or equal to 10.
Concomitant use with strong CYP3A inhibitors: tolvaptan is contraindicated in patients taking strong inhibitors of the enzyme CYP3A, such as ketoconazole, itraconazole, clarithromycin, ritonavir, and others, as these drugs can increase tolvaptan blood levels and increase the risk of adverse effects.
Anuria: tolvaptan should not be used in patients who are unable to produce urine (anuria).
Hypovolemic hyponatremia: tolvaptan is not recommended for the treatment of hypovolemic hyponatremia, which is a type of hyponatremia caused by fluid loss.
Pregnancy: tolvaptan is classified as a pregnancy category C medication, meaning that it may be harmful to a developing fetus and should be used with caution during pregnancy.
Breastfeeding: tolvaptan is not recommended for use in breastfeeding mothers, as it may be excreted in breast milk and could potentially harm a nursing infant.

Caution:

Moderate liver impairment: tolvaptan should be used with caution in patients with moderate liver impairment, such as those with a Child-Pugh score of 7-9.
Concomitant use with CYP3A inducers: tolvaptan should be used with caution in patients taking drugs that induce the enzyme CYP3A, such as rifampin, carbamazepine, phenytoin, and others, as these drugs can decrease tolvaptan blood levels and reduce its effectiveness.
Dehydration: tolvaptan may increase urine output, which can lead to dehydration.
Hyperkalemia: tolvaptan can increase serum potassium levels, particularly in patients with underlying kidney disease. Patients should be monitored for hyperkalemia, and the dose of tolvaptan may need to be adjusted accordingly.
Hypotension: tolvaptan can cause a decrease in blood pressure, particularly in patients with underlying heart disease or taking medications that lower blood pressure. Patients should be monitored for hypotension, and the dose of tolvaptan may need to be adjusted accordingly.
Elderly patients: Elderly patients may be more sensitive to the effects of tolvaptan and may be at increased risk of adverse effects.
Hyponatremia due to SIADH: tolvaptan may be less effective in treating hyponatremia caused by the syndrome of inappropriate antidiuretic hormone secretion (SIADH).

Comorbidities:

Heart failure: tolvaptan may be used in patients with heart failure and hyponatremia.
Liver cirrhosis: Hyponatremia is a common complication of liver cirrhosis, and tolvaptan may be used to treat this condition. However, tolvaptan is contraindicated in patients with severe liver impairment.
Syndrome of inappropriate antidiuretic hormone secretion (SIADH): tolvaptan may be used to treat hyponatremia caused by SIADH, although it may be less effective in this condition.
Cancer: Some types of cancer, particularly lung cancer, can cause hyponatremia. tolvaptan may be used in these patients, although it is not approved specifically for this indication.
Central nervous system disorders: Certain conditions that affect the CNS, such as meningitis, encephalitis, or brain tumors, can cause hyponatremia. tolvaptan may be used to treat hyponatremia in these patients.

Pregnancy consideration: pregnancy category: not assigned

Lactation: It is not known whether tolvaptan is excreted in human milk.

Pregnancy category:

Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.
Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women.
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.
Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women.
Category N: There is no data available for the drug under this category.

Pharmacology:

tolvaptan is a selective vasopressin V2 receptor antagonist, which means that it blocks the action of the hormone vasopressin on the V2 receptors in the kidneys. Vasopressin regulates the body’s water balance by increasing water reabsorption in the kidneys. By blocking the action of vasopressin on the V2 receptors, tolvaptan promotes water excretion and increases urine output, leading to an increase in serum sodium levels.

tolvaptan is rapidly absorbed after oral administration, with peak plasma concentrations reached within 2-4 hours. The drug is metabolized by liver, primarily by the enzyme CYP3A4, and is eliminated mainly via the feces. tolvaptan has a half-life of about 12-15 hours in healthy individuals, but this may be prolonged in patients with liver or kidney impairment.

tolvaptan is primarily used for the treatment of hyponatremia, which is a condition characterized by low sodium levels in the blood. Hyponatremia can be caused by a variety of underlying conditions, such as heart failure, liver cirrhosis. tolvaptan can be effective in increasing serum sodium levels and improving symptoms in patients with hyponatremia, although it is associated with a risk of liver injury and should be used with caution in patients with liver impairment.

Pharmacodynamics:

tolvaptan is a selective vasopressin V2 receptor antagonist that works by blocking the action of arginine vasopressin (AVP), a hormone that regulates the balance of water and electrolytes in the body. By blocking the AVP receptors in the renal collecting ducts, tolvaptan increases water excretion and decreases the concentration of electrolytes such as sodium in the urine.

The pharmacodynamics of tolvaptan are primarily related to its effect on the renal system. tolvaptan works by inhibiting the reabsorption of water in the kidney, leading to an increase in urine output and a decrease in plasma sodium concentration. This effect is dose-dependent and can be observed within hours of administration.

In patients with hyponatremia (low sodium levels in the blood), tolvaptan has been shown to increase serum sodium levels by promoting the excretion of excess water.

Pharmacokinetics:

Absorption

tolvaptan is rapidly absorbed after oral administration, with peak plasma concentrations reached within 2 to 4 hours. Food can delay the absorption of tolvaptan but does not significantly affect its bioavailability.

Distribution

tolvaptan is highly protein-bound (99%) and has a large volume of distribution, indicating that it is extensively distributed throughout the body.

Metabolism

tolvaptan is extensively metabolized by cytochrome P450 (CYP) enzymes, primarily CYP3A4 and CYP2C9. The major metabolites of tolvaptan are the 1-O-glucuronide and the 6-hydroxymethyl metabolites, both of which are pharmacologically inactive.

Elimination and excretion

tolvaptan is primarily eliminated by renal excretion, with about 70% of a dose excreted unchanged in the urine. The remainder of the dose is eliminated in the feces (21%) and through metabolism (9%).

Administration:

tolvaptan should be taken with water, and food does not significantly affect its absorption.
The recommended starting dose of tolvaptan for the treatment of hyponatremia is typically 15 mg once daily. The dose can be increased to 30 mg once daily after at least 24 hours if the serum sodium concentration does not increase by at least 4 mEq/L or if symptoms of hyponatremia persist.
The maximum recommended daily dose of tolvaptan is 60 mg.
tolvaptan should be taken at the same time each day to maintain consistent drug levels in the blood.
tolvaptan should not be crushed or chewed, and the tablets should be swallowed whole.
tolvaptan may interact with other medications, so patients should inform their healthcare provider of all medications they are taking, including over the counter and herbal supplements.
Patients should be monitored regularly for changes in serum sodium concentration and for signs of liver dysfunction, especially during the first 18 days of treatment, as tolvaptan has been associated with an increased risk of hepatotoxicity.
tolvaptan should be discontinued if there is evidence of liver injury or if the serum alanine aminotransferase (ALT) level increases to three times the upper limit of normal.

Patient information leaflet

Generic Name: tolvaptan

Pronounced: [ tol-VAP-tan]

Why do we use tolvaptan?

Hyponatremia: tolvaptan is FDA-approved for the treatment of euvolemic or hypervolemic hyponatremia associated with cirrhosis, heart failure, and the syndrome of antidiuretic hormone secretion (SIADH). It works by increasing the excretion of free water and reducing water retention, leading to an increase in serum sodium levels.
Autosomal dominant polycystic kidney disease (ADPKD): tolvaptan has also been approved for the treatment of ADPKD, which is a genetic disorder characterized by the growth of numerous cysts in the kidneys. tolvaptan has been shown to slow the progression of kidney disease in patients with ADPKD by reducing the growth of kidney cysts.
Ascites: tolvaptan may be used off-label for the treatment of ascites, which is the accumulation of fluid in the abdominal cavity that can occur in patients with liver cirrhosis. tolvaptan can reduce fluid accumulation and improve symptoms in some patients with ascites.
Heart failure: tolvaptan has been investigated for its potential use in the treatment of acute decompensated heart failure, but its use in this context is not yet FDA-approved.

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tolvaptan

Brand Name :

Samsca, Jynarque

Synonyms :

tolvaptan

Class :

Vasopressin Antagonists; Vasopressin-Related

Dosage Forms & Strengths

tablet (Samsca)

30mg

15mg

tablet (Jynarque)

90mg

60mg

45mg

30mg

15mg

Safety and efficacy not established

Refer to the adult dosing regimen

DRUG INTERACTION

tolvaptan

&

Pembrolizumab / Berahyaluronidase
Bumetanide Intranasal
Gemcitabine intravesical
Rilzabrutinib
Zopapogene
Aceclidine
aluminium hydroxide
benzralizumab (Rx)
Rituximab
Trimetrexate Glucuronate
Mirdametinib
Suzetrigine
Potassium acid phosphate
Acellular Tissue Engineered Vessel
crinecerfont (pending approval from FDA)
Revumenib
pembrolizumab (Rx)
azathioprine (Rx)
Gemcitabine (Rx)
Seladelpar
Atezolizumab / Hyaluronidase-tqjs
Axatilimab-csfr
Afamitresgene Autoleucel
Lazertinib
Ocrelizumab / Hyaluronidase ocsq
Lebrikizumab
naloxone intranasal
clomiphene
patisiran
imetelstat
phenylephrine ophthalmic
myoinositol
vasicinone
soda lime
fisetin
Reynoutria Japonica
Coco Monoethanolamide
Betadex
lithopone
cyperus rotundus
papaya juice
1-naphthaleneacetic acid
Nordazepam
Glechoma hederacea
Alternanthera sessilis
nicofetamide
napthol asol
cocamidopropyl betaine
musa x paradisiaca
dicyclomine/mefenamic acid
Sorghum
Manganese citrate
tovorafenib
mefenamic acid/paracetamol
eschscholzia californica
canna indica root
tranexamic acid/mefenamic acid
dexverapamil
sitogluside
secalciferol
cefatrizine
Sedum Acre
Flurogestone
Fluocortin
Bifendate
piprozolin
aminacrine undecylate
ethylenediamine mandelate
pelubiprofen
hesperetin
butethamine
epitiostanol
androstenediol
Nitroxoline
Iocarmic acid
Capobenic acid
dordaviprone (investigational drug)
Vitexin
Friluglanstat (investigational drug)
scorias spongiosa
Luseogliflozin
indoxacarb
prademagene zamikeracel
fidanacogene elaparvovec-dzkt
albifylline
idanpramine
araneus diadematus
Sulfamazone
Lycosa tarantula
malotilate
Ethacizine
Namilumab
Latrunculin B
stachyose
platinic oxide
iopronic acid
calcium chloride / potassium chloride/lactic acid/ sodium chloride/sodium hydroxide/sodium lactate solution
citric acid/ sodium bicarbonate/ sodium carbonate anhydrous
vadadustat
permethrin medical grade cis/trans isomers 25/75
lutetium, isotope of mass 177
human normal immunoglobulin
sacrosidase
apadamtase alfa, recombinant
acetyl hexapeptide-8 amide
pemivibart (Investigational)
govorestat
Zanidatamab
sotatеrcеpt
MV 140 vaccine
leuprorelin implant
cinchocaine hydrochloride/fluocortolone hexanoate/fluocortolone pivalate
Beautyberry
risedronate/calcium/vitamin D3
rhubarb extract/senna leaf/sulphur purified/wood charcoal
boric acid/kaolin/methyl salicylate/peppermint oil/thymol
docosahexaenoic acid/eicospentaenoic acid
aluminium hydroxide/magnesium hydroxide/simethicone
gentamicin/hydrocortisone
succinylcholine
sinefungin
letibotulinumtoxinA
coal tar/coconut oil/salicylic acid
camphor/camphor oil white/capsicum oleoresin /menthol/methyl salicylate
thioglycolic acid
acetic acid auricular
roluperidone
hydrocortisone/crotamiton topical
nystatin/chlorhexidine
aluminium chloride hexahydrate
ketoprofen topical
Chlormethine
podophyllotoxin
urea/lactic acid
autologous chondrocytes implant
afelimomab
gepotidacin
fludroxycortide
fentanyl transdermal
erythromycin/zinc acetate
dibotermin alfa powder
desferrioxamine mesilate
choline salicylate/magnesium salicylate
castor oil/peru balsam/trypsin
betamethasone/dexchlorpheniramine maleate
benzalkonium chloride solution/cetrimide
barzolvolimab
ascorbic acid / calcium laevulinate / nicotinamide / calcium pantothenate / calcium chloride / riboflavine / pyridoxine hydrochloride / thiamine hydrochloride
argipressin
arachis oil refined/chlorobutanol hemihydrate
arachis oil/eucalyptol/nutmeg oil/terpineol
ammonium chloride/diphenhydramine hydrochloride/levomenthol
amino acid mixture d / calcium chloride dihydrate / glucose monohydrate / glycine / magnesium chloride hexahydrate / olive oil / potassium chloride / sodium acetate trihydrate / sodium glycerophosphate pentahydrate / soya-bean oil
biotin/colecalciferol/copper (ii)sulfate dried/ cyanocobalamine/ dl-alpha tocopherol acetate/dibasic calcium phosphate anhydrous/folic acid/iron (ii)sulfate dried/ lecithin/ magnesium sulfate dried/ nicotinamide/ pyridoxine hydrochloride/ riboflavin
ampicillin sodium / cloxacillin sodium
undecylenic acid, undecylenate salts, zincundecate
omeprazole/sodium bicarbonate
efgartigimod alfa/hyaluronidase
xylometazoline/ipratropium
cefepime and enmetazobactam
isotonic sodium chloride
bee venom allergen injection
fentanyl intranasal
alglucosidase alfa
triprolidine/pseudoephedrine
pegademase bovine
castor oil and peru balsam
camphor/eucalyptus oil/menthol
oxyquinoline/sodium lauryl sulfate
somatorelin
menotrophin injection
menadiol
hylan g-f 20
cefepime and taniborbactum
water avens
camphor/menthol
acoramidis
elafibranor
arrowroot
miconazole nitrate/hydrocortisone
vildagliptin/metformin
dobesilic acid
aroxybutynin and atomoxetine
hygromycin
linvoseltamab
nemolizumab
aceprometazine
limaprost
oxazolam
trimegestone
teceleukin
beauty berry
dinotefuran
imiprothrin
transfluthrin
thymalfasin
technetium Tc 99m tilmanocept
glepaglutide
marstacimab
pixantrone
Andiroba
arabinoxylan
arenaria rubra
etripamil
jequirity
jiaogulan
dusquetide
rolipram
tradipitant
sinfungin
diclofenac/omeprazole
brinzolamide and timolol maleate
wormseed
wormwood
wood sorrel
carmellose sodium
ibandronic acid
cinnarizine and dimenhydrinate
ursodeoxycholic acid
rhubarb extract/salicylic acid
butamirate citrate
fumitory
taheebo
uva ursi
vervain
coleus
coltsfoot
crampbark
plantain
potassium nitrate and silver nitrate
gelsemium
gentian
glucomannan
walnut
meadowsweet
midomafetamine
pennyroyal
periwinkle
betony
bitter orange
bladderwrack
bloodroot
emu oil
garcinia
yellow dock
burdock
dehydroepiandrosterone
aucubin
jasmone
resacetophenone
ecamsule ditriethanolamine
feclobuzone
fenoprop triethanolamine
verdyl acetate
caffeic acid
cyclamen aldehyde
dicetyldimonium chloride
wogonin
impacarzine
laurylpyridinium chloride
stepronin
matrine
sakuranin
cannabichromene
sandalore
sabinene
oxypaeoniflora
ethylhexyl pelargonate
acrylonitrile
allyl alcohol
dipalmitoylethyl hydroxyethylmonium methosulfate
butidrine
clothiapine
propanediol dicaprylate
buchu
undecanol
enilconazole
xymenynic acid
angelica
nizubaglustat
resomelagon
ulecaciclib
apple cider vinegar
bacopa
barley grass
dandelion
deer velvet
dolomite
bugleweed
bupleurum
glyceryltrinitrate
pociredir
asnuciclib
actalycabtagene autoleucel
butantan–dengue vaccine
travoprost/timolol
furosemide/potassium chloride
amylamine
jaborandi
patritumab deruxtecan
jackfruit
sterculia
ascorbigen
ashitaba
androstenetrione
andrachne
cosibelimab
racecadotril
neomycin/chlorhexidine
octocog alfa
cetrimide
ispaghula husk
polyhexanide
octenidine
polygeline
heparinoid
jewelweed
boldo
anizatrectinib
alpinia
henbane
cynanchum vincetoxicum root and sulfur
boditrectinib
izumerogant
zavondemstat
abuta
fadogia agrestis
fly agaric mushroom
meptazinol
methoxyflurane
tramadol/dexketoprofen
betaine/polyhexanide
filgotinib
inosine acedoben dimepranol
alverine citrate
hyoscine butylbromide
senna+ ispaghula
cabbage palm
cajeput oil
calanus oil
calamint
canada balsam
carnosine
alverine citrate/simeticone
dihydroartemisinin/piperaquine
mebeverine/ispaghula
calcipotriol
tacalcitol
triethyl citrate/ethyl linoleate
sodium dilauramidoglutamide lysine
fazamorexant
avibactam tomilopil and ceftibuten
drostanolone
tigilanol tiglate
isorhynchophylline
rhynchophylline
crisugabalin
epigallocatechin gallate
clomocycline
corynoxeine
isocorynoxeine
Culmerciclib
Neladenoson
ambrein
hexylcaine
phensuximide
resencatinib (investigational)
rolusafine
pumecitinib
arhalofenic acid
berdazimer sodium
benzquinamide
clidinium
sulfametopyrazine
fulzerasib (Investigational Drug)
rovadicitinib (Investigational Drug)
Upleganan (Investigational Drug)
menthyl ethylamido oxalate
quaternium-90 montmorillonite
unecritinib (investigational drug)
etohexadiol
guaiol
proximadiol
verdinexor
sofnobrutinib
talbutal
ethoxzolamide
propiomazine
enprofylline
phenmetrazine
merigolix
pralurbactam
neracorvir
vonifimod
apaziquone hydroquinone
darizmetinib
zandelisib
xininurad
ritivixibat
amiselimod phosphate (investigational drug)
emzeltrectinib (investigational drug)
ficonalkib
cinalukast
ulobetasol
candoxatril
nitrofural
acetyldigitoxin
bentiromide
dextrothyroxine
chlorotrianisene
remikiren
pipobroman
vidarabine
immune globulin intravenous, human-stwk
spermine
serine
N-acetyl glucosamine
valine
adenine
asparagine
citrulline
adinazolam
interferon alfacon-1
interferon alfa-n1
felypressin
birch triterpenes
pyridoxal phosphate
technetium Tc-99m arcitumomab
beta-alanine
dihomo-gamma-linolenic acid
urea/hydrocortisone
R21/Matrix-M vaccine
povidone-iodine (ophthalmic)
pheniramine
hydrocortisone rectal
chloroxylenol/pramoxine/zinc acetate
chloroxylenol/pramoxine
dextrose/sucrose/vitamin C/zinc sulphate
furazolidone/metronidazole/dicyclomine
ergocalciferol (vitamin D2)
benoxaprofen (discontinued)
teicoplanin
carbomer
chromic chloride / iron (ii) chloride tetrahydrate / potassium iodide / manganese chloride / sodium fluoride / sodium selenite pentahydrate / sodium molybdate dihydrate / zinc chloride/ cupric chloride
bufylline
lidocaine/prilocaine
opium tincture, squill oxymel
dibrompropamidine
metronidazole/tetracycline/bismuth subsalicylate
agnus- castus
velaglucerase alfa
alendronic acid / colecalciferol
bimatoprost / timolol
efbemalenograstim alfa
dried ferrous sulfate/folic acid
dried ferrous sulfate / sodium ascorbate
nirogacestat
soya-bean oil, medium-chain triglycerides
demeclocycline hydrochloride and triamcinolone acetonide
fusidic acid / hydrocortisone acetate
macrogol
storax, benzoin
nomegestrol acetate/estradiol
flumetasone pivalate/ clioquinol
berdazimer topical (Pending FDA Approval)
buflomedil
butobarbital
andexanet alfa
methoxypolyethylene glycol-epoetin beta
viscum abietis
pramoxine vaginal
bupivacaine implant
cromolyn sodium, inhaled
pneumococcal vaccine 20-valent
bimatoprost ophthalmic implant
tick-borne encephalitis vaccine
chloroprocaine ophthalmic
travoprost intraocular implant (Pending FDA approval)
typhoid polysaccharide vaccine
sodium phosphate
human papillomavirus vaccine, nonavalent
peanut immunotherapy epicutaneous (FDA approval pending)
cromolyn sodium, intranasal
red blood cells(Blood component)
oral mucoadhesive
clindamycin vaginal
whole blood (Blood Component)
fibrinogen/thrombin
levothyroxine/liothyronine
ipratropium intranasal
metronidazole vaginal
cyamemazine
brinase
reviparin
ulinastatin
saruplase
acepromazine
emylcamate
methionine
amino acids and electrolytes in dextrose with calcium
slippery elm
camostat
hemoglobin crosfumaril
moperone
chlormidazole
brilaroxazine
palopegteriparatide
diazepam buccal
benegrastim (pending for FDA approval)
COVID-19 vaccine, adjuvanted-Novavax
vestronidase alfa-vjbk
tebipenem (Pending FDA Approval)
tislelizumab (Pending FDA Approval)
zolbetuximab (Pending FDA Approval)
zoliflodacin (pending FDA approval)
zibotentan and dapagliflozin
fluorine F18 DCFPyL
debamestrocel
givinostat
amubarvimab and romlusevimab(Pending FDA Approval)
sabizabulin(Pending FDA approval)
fexapotide(Phase 3 Clinical trial)
diatrizoic acid
drotaverine
diethyl phthalate
enclomiphene
epalrestat
ethamsylate
flupirtine
imidurea
sodium glycolate
feracrylum
ethacridine
furazolidone/metronidazole
ozagrel hydrochloride
leptazol
l-glutamic acid /vitamin B complex
etizolam
etizolam/propranolol
ethoheptazine citrate
etophylline and theophylline
etophylline
finger millet
drotaverine/mefenamic acid
dichloroxylenol
pneumococcal 7-valent vaccine
diclofenac and metaxalone
dipivefrin ophthalmic
enbucrilate
potassium citrate and citric acid
potassium gluconate
aclarubicin
alfuzosin/dutasteride
adrenochrome monosemicarbazone
selenium sulfide topical
sertaconazole
amorolfine cream
amsacrine
amylmetacresol
sulfonated phenolics in aqueous solution
technetium Tc-99m sulfur colloid
raltitrexed
romiplostim
acediasulfone
azulene
acebrophylline
clonazepam/escitalopram oxalate
allylestrenol
andrographolide
artemotil
technetium Tc-99m sestamibi
rubidium Rb-82
somapacitan
sodium sulfate, magnesium sulfate and potassium sulfate
almitrine
gramicidin
nikethamide
technetium Tc-99m sodium pertechnetate
betiatide
prilocaine/epinephrine
amlexanox
acetaminophen/salicylamide/phenyltoloxamine
neomycin topical
zilucoplan
antazoline and xylometazoline
toripalimab
iron isomaltoside
meningococcal A C Y and W polysaccharide tetanus toxoid conjugate vaccine
meningococcal A C Y and W-135 diphtheria conjugate vaccine
tetradecyl Sulfuric Acid
benzoyl peroxide, clindamycin phosphate, adapalene
ethylephedrine
actarit
pyrantel tartrate
tenofovir disoproxil fumarate or tenofovir DF
melitracen
amitriptylinoxide(Phase 4 Clinical Trials)
threonine
ditiocarb zinc
epicriptine
levallorphan
kinetin
laurocapram
pentagastrin
parthenolide
nicoboxil
protionamide
prulifloxacin
proscillaridin
tizanidine and rofecoxib
tolnaftate, gentamicin, chinoform and betamethasone valerate
pine bark extract
pipenzolate methylbromide
bephenium hydroxynaphthoate
niclosamide
pyrvinium
pipenzolate methylbromide/phenobarbitone
piracetam/ginkgo biloba/vinpocetine
benzyl benzoate/disulfiram
benzyl benzoate
loperamide/simethicone
piroctone olamine
sodium fusidate
piroxicam topical/capsaicin/menthol/methyl salicylate
sodium metabisulfite
sodium lauryl sulfate
taspoglutide
glyclopyramide
tolnaftate, gentamicin, iodochlorohydroxyquinoline, chlorocresol, betamethasone valerate
serratiopeptidase
sodium antimony gluconate
triamterene / benzthiazide
tribenoside / lidocaine
triclocarban
triprolidine/dextromethorphan
vitamins/minerals/omega-3 Fatty acids
soyabean oil
sucralfate/oxethazaine
sucralfate/tinidazole/povidone iodine
sodium cromoglycate
aloe vera/liquid paraffin/white soft paraffin
aloe vera/jojoba oil/vitamin E
allantoin/triclosan/vitamin e/zinc oxide
alpha-Lipoic acid/minerals/multivitamins
alprazolam/paracetamol
alprazolam/melatonin
azithromycin/ambroxol
atorvastatin/clopidogrel/aspirin
aceclofenac, paracetamol and serratiopeptidase
alfacalcidol, vitamin B-complex, minerals and antioxidants
alpha- lipoic acid, vitamin b complex and vitamin c
alpha-galactosidase and simethicone
alpha-galactosidase, amylase, proteases, lipase and lactase
amikacin and cefepime
aminophylline, ephedrine and phenobarbitone
artesunate, sulphadoxine and pyrimethamine
finasteride/tamsulosin
flavoxate/ofloxacin
fenofibrate/metformin
lignocaine, hydrocortisone topical and allantoin
linoleic acid and sodium lactate
troxerutin
meclizine/nicotinic acid
mecobalamin/ginkgo Biloba
spirulina
loperamide and furazolidone
ketoconazole/cetrimide
ketoconazole/zinc pyrithione
lercanidipine/atenolol
levocetirizine/montelukast/ambroxol
levarterenol
levocetirizine/phenylpropanolamine
indapamide/amlodipine
itopride/methyl polysiloxane
mebendazole/levamisole
eberconazole/mometasone
gliclazide/metformin/pioglitazone
fluconazole/tinidazole
haemocoagulase
halometasone
hesperidin
imipramine/chlordiazepoxide
idebenone / l-arginine / zinc sulphate/selenium/proanthocyanidin
mecobalamin and piracetam
mesterolone
mosapride and pantoprazole
atorvastatin, co enzyme q10, vitamin e, zinc, and selenium
azithromycin and benzalkonium chloride
beta carotene, vitamin c, vitamin e, minerals, lutein, eicosapentaenoic acid, docosahexenoic acid and vit b12
alpha-galactosidase
aloe vera gel/vitamin e/lactic acid
aloe vera gel/jojoba/vitamin e/glycerine
famotidine and domperidone
faropenem medoxomil
nedosiran
fluconazole/ornidazole/azithromycin
ebastine/montelukast
eberconazole
dienogest/estradiol valerate
ambroxol/salbutamol
benzoic acid/salicylic acid/ichthammol/ triamcinolone acetonide
desloratadine/ambroxol
dexibuprofen/paracetamol
atorvastatin/ramipril
diastase
diastase and simethicone
diazepam and propranolol
dexrabeprazole / domperidone
dexrabeprazole
dexketoprofen /paracetamol
beta carotene/vitamin C/minerals
aloe vera gel/urea
aloe vera gel/glycerine
alpha-lipoic acid/benfotiamine/chromium/folic acid/mecobalamin / vit b6
alprazolam/propranolol
alprazolam /sertraline
ibuprofen/dextropropoxyphene
ambroxol/cetirizine/phenylephrine/ guaiphenesin/menthol
dextropropoxyphene/dexchlorpheniramine maleate/bromhexine
promegestone
batroxobin
bencyclane
benfluorex
acetylpheneturide
abarelix
abetimus
naftidrofuryl
nalorphine
oxiracetam
letosteine
lafutidine
leuprorelin
levodropropizine
glutaral
losartan/ramipril
gallopamil
lanatoside c
lauromacrogol
gestodene
aceclofenac/methyl salicylate/menthol/linseed oil/capsaicin
aceclofenac/paracetamol/tizanidine
alginic acid/magaldrate/simethicone
aceclofenac/paracetamol
aceclofenac/rabeprazole
alginic acid
pantoprazole and domperidone
urokinase
rimiterol
olanzapine/fluoxetine
normethadone/hydroxyephedrine
myrtol
moxonidine
propylhexedrine
sodium hypochlorite solution
sodium chloride/sodium citrate
Hepatitis B Vaccine (Recombinant [Adjuvanted])
Hepatitis B Vaccine (Recombinant)
aceclofenac and serratiopeptidase
levosulpiride
niaprazine
tromantadine
trimetazidine
vinburnine
mizoribine
molgramostim
mosapride
eugenol
tolperisone
etamsylate
etynodiol
mizolastine
metenolone
reproterol
rebamipide
mephenoxalone
metandienone
furosemide/spironolactone
hydroxycarbamide
tenonitrozole
fenoverine
fenquizone
tiapride
tibolone
furazolidone
furosemide & amiloride
fosfestrol
fluclorolone
flubendazole
tertatolol
tetracosactide
tetryzoline
tolciclate
trapidil
troxipide
temoporfin
telbivudine
teprenone
hexamidine
mebhydrolin
mepartricin
fencamfamin
medazepam
theodrenaline
thiamazole
thiocolchicoside
psilocybin
veralipride
pyritinol
opipramol
oprelvekin
betamethasone + gentamicin
betamethasone + neomycin
betamethasone + salicylic acid
oxedrine
bopindolol
orgotein (investigational)
oxaceprol
ormeloxifene
bevantolol
bifemelane
clebopride
demoxytocin
cicletanine
cefsulodin
chlortalidon
sisomicin
somatrem
carbazochrome
caroverine
cathine
ipriflavone
isepamicin
silymarin
simethicone
sermorelin
diloxanide
dimethindene
diosmin/hesperidin
calamine
canrenone
captodiame
imidapril
cefetamet
cefodizime
cefoperazone + sulbactam
ivermectin + albendazole
serrapeptase
bromisoval
beraprost
pridinol
proglumide
bamipine
barnidipine
bamifylline
benzbromarone
betamethasone/fusidic acid
para-chlorophenol
pantethine
nomifensine
pemoline
parnaparin
pentolinium
nialamide
novobiocin
nicergoline
octocrylene
octisalate
oftasceine
oxolamine
oxyphencyclimine
penfluridol
pentoxyverine
phenoxymethylpenicillin
picloxydine
pilsicainide hydrochloride
piperazine
pirarubicin
policresulen
prifinium bromide
prethcamide
pristinamycin
pirenzepine
piribedil
pimethixene
pargyline
phosphatidyl choline
phthalylsulfathiazole
phytomenadione
pranlukast
pinazepam
oxyphenonium
noxytiolin
periciazine
pethidine
phenindamine
histidine
isoleucine
proline
lauric acid
lymecycline
hypromellose
abiraterone acetate and niraparib
ichthammol
levamisole
naftazone
nefopam
oxprenolol
oxybuprocaine
elranatamab-bcmm
lapyrium
isoaminile
iotrolan
mazindol
masoprocol
lypressin
meradimate
molsidomine
monobenzone
mequinol/gluconolactone/ lactobionic acid/ arbutin
medifoxamine
mebutamate
metergoline
methantheline
methdilazine
metocurine
micronomicin
metaraminol
mephenesin
menadione
medrysone
metixene
levobetaxolol
guaiacol glycerol ether
eucalyptol
sodium tetradecyl sulfate
sugammadex
carbetocin
certoparin
chlorcyclizine/pseudoephedrine
cephapirin
indecainide
iobitridol
iomeprol
chlorphenesin
msud analog
msud maxamum
iceland moss
glutethimide
hexachlorophene
haloprogin
deferoxamine
ethchlorvynol
dexpanthenol topical
etilefrine
deslanoside
carbocromen
diazolidinylurea
dibenzepin
etofamide
guanoxan
halazepam
guanadrel sulfate
dapiprazole
soapwort
debrisoquine
l-tryptophan
chlormerodrin
chlorquinaldol
cetrimonium
carbocisteine
chlorcyclizine/codeine
technetium Tc-99m tetrofosmin
technetium Tc-99m disofenin
technetium Tc-99m gluceptate
technetium Tc-99m labeled red blood cells
amylmetacresol/dextromethorphan hydrobromide
anileridine phosphate
pyrethrins
pyrantel pamoate
quinagolide
spiramycin
standard hyperkalemic cardioplegia solution
technetium tc-99m mertiatide
technetium tc-99m medronate
bemotrizinol / bisoctrizole
benfotiamine
bemotrizinol + titanium dioxide + zinc oxide
technetium Tc-99m oxidronate
technetium Tc-99m pentetate
technetium Tc-99m pyrophosphate
benziodarone
octinoxate/bisoctrizole
bicisate dihydrochloride
technetium Tc-99m bicisate
norelgestromin/ethinyl estradiol
norgestimate/ethinyl estradiol
ximelagatran (investigational)
xamoterol
trioxsalen
poly-urea urethane
rilmenidine
pemirolast
oxitriptan
beclomethasone, intranasal
thimerosal
camphor gel
camphor
mumps virus vaccine, live
rubella virus vaccine, live
aluminum chloride (dental)
alum irrigation
framycetin, phenylephrine, and gramicidin
ombitasvir, paritaprevir, ritonavir, and dasabuvir
olipudase alfa
etonogestrel/ethinyl estradiol
mycophenolate
fluoroestradiol F 18
donor organ cardioplegia solution
fluciclovine F 18
fusidic acid (ophthalmic)
fusidic acid and hydrocortisone
framycetin, dexamethasone, and gramicidin
fludeoxyglucose F-18
fluorouracil/salicylic acid
indium In-111 oxyquinoline
indium In-111 pentetreotide
indium In-111 capromab pendetide
lusutrombopag
mitomycin (ophthalmic)
mifepristone and misoprostol
minoxidil (systemic)
methyl aminolevulinate (topical)
methyl folate, methylcobalamin, and acetylcysteine
ciclesonide/formoterol/tiotropium
nedocromil (Oral Inhalation)
batefenterol (Investigational)
neostigmine and glycopyrrolate
nepafenac ophthalmic
netupitant/palonosetron
meperidine and promethazine
mepivacaine and levonordefrin
maltodextrin
medical cannabis
medium chain triglycerides
mometasone/glycopyrrolate (glycopyrronium)/ indacaterol
moxifloxacin ophthalmic
neomycin/fluocinolone
nadroparin
iodine I-125 iothalamate
amikacin liposome (oral inhalation)
bupivacaine liposome
natamycin
lopinavir and ritonavir
lysine
macitentan and tadalafil
mitomycin pyelocalyceal
moclobemide
mometasone and indacaterol
efinaconazole
blue-green algae
indocyanine green
follitropin beta
lumasiran
glycerin/lidocaine
edrophonium/atropine
indigo carmine
lutropin alfa
instant glucose/intravenous dextrose
iobenguane I-123
ixekizumab
isosulfan blue dye
levofloxacin ophthalmic
levonorgestrel oral/ferrous bisglycinate/ ethinylestradiol
ethinyl estradiol/levonorgestrel transdermal
hydroquinone
hydroxypropyl methylcellulose
icodextrin
lipid emulsion (soybean, medium-chain triglyceride, olive, and fish oils; [SMOF])
iodinated I 125 albumin
iodinated I 131 albumin
lipid emulsion (plant oil-based)
levonorgestrel intrauterine
levonorgestrel/ethinyl estradiol
lactic acid and sodium-PCA
lactated Ringer solution
ketotifen (systemic)
lanolin
leuprolide and norethindrone
levodopa and benserazide
gonadorelin acetate
hemodialysis solutions
nirsevimab
gentian violet
gallium ga-68 dotatate
fusidic acid and betamethasone
gallium citrate Ga-67
gadopentetate dimeglumine
gadofosveset
follitropin delta
follitropin alfa and lutropin alfa
follitropin alfa
rocatinlimab
grass pollens allergen extract
flotufolastat F18
fluorescein ophthalmic
barium
balanced salt solution
air polymer type A intrauterine device
clodronate
bentoquatam
clobetasone
alfacalcidol
citric acid/glucono-delta-lactone/magnesium carbonate
benzoin
desirudin
immune globulin IV (IGIV)
dequalinium
pseudoephedrine/desloratadine
clofedanol
cyproterone and ethinyl estradiol
dextranomer and hyaluronic acid or derivatives
diatrizoate meglumine and diatrizoate sodium
glucosamine sulfate, chondroitin sulfate and Msm
squill
gotu kola
blessed thistle
bitter melon
apraclonidine
chlophedianol/dexbrompheniramine/pseudoephedrine
wild jujube
chitosan
cilazapril/hydrochlorothiazide
dexbrompheniramine and phenylephrine
diethylene triamine penta-acetic acid
dexchlorpheniramine and pseudoephedrine
lily of the valley
diflucortolone
corydalis
lemon balm
MSM
calcium polystyrene sulfonate
caprylidene
peppermint oil
efavirenz/lamivudine/tenofovir DF
emtricitabine/tenofovir DF /efavirenz
dutasteride/tamsulosin
milk thistle
centaury
horseweed
lycopus
agrimony
alfalfa
kava
cetrorelix
cetylpyridinium
chlophedianol and dexbrompheniramine
betahistine
choline C-11
boric acid vaginal suppository
aluminum acetate
aluminum chloride hexahydrate
14-C urea breath test
absorbable collagen
valoctocogene roxaparvovec-rvox
amlodipine and celecoxib
aspirin and omeprazole
azilsartan and chlorthalidone
landiolol (Pending FDA approval)
isosorbide dinitrate/hydralazine
losartan/hydrochorothiazide
udenafil
dextromethorphan/quinidine
onasemnogene abeparvovec
orphenadrine/aspirin/caffeine
Trace elements
sodium phenylbutyrate/ taurursodiol
fish oil triglycerides
infant formula
glutamine
chloroquine phosphate
afatinib
quinidine gluconate
methylergonovine
prothrombin complex concentrate, human
BCG intravesical live
capivasertib
cedazuridine
carbonyl iron
iron dextran complex
lovotibeglogene autotemcel (FDA Approval Pending)
sodium benzoate/sodium phenylacetate
mineral oil otic
zolmitriptan transdermal
midazolam intranasal
fosinopril/hydrochlorothiazide
caplacizumab
arginine
sodium phenylbutyrate
meloxicam/rizatriptan
manganese
acetaminophen/pamabrom/pyridoxine
varicella zoster immune globulin, human
amitriptyline/perphenazine
narsoplimab (Pending FDA Approval)
amlodipine/perindopril
imiglucerase
canagliflozin/metformin
tafamidis meglumine
somatrogon-ghla
glimepiride/rosiglitazone
becaplermin
lithium
loxapine inhaled
nicotine transdermal
tixagevimab and cilgavimab (Investigational)
muromonab CD3
ansuvimab
coal tar bath products
fibrin sealant
arimoclomol (FDA Approval Pending)
varenicline intranasal
aducanumab
oxycodone/naloxone
ritlecitinib
sodium polystyrene sulfonate
calcipotriene/betamethasone
calcium hydroxylapatite
cantharidin topical
doxepin cream
clocortolone
formaldehyde topical
sodium sulfide topical
collagenase
selegiline transdermal
foscarbidopa/foslevodopa (FDA approval pending)
saxagliptin/metformin
linagliptin/metformin
linzagolix (FDA approval pending)
efgartigimod/hyaluronidase SC
Elamipretide
rozanolixizumab
diazoxide
glimepiride/pioglitazone
cipaglucosidase alfa
dihydroergotamine intranasal
delandistrogene moxeparvovec
beremagene geperpavec
hyaluronic acid and derivatives
hyaluronic acid, non-animal stabilized
eplontersen (FDA Approval Pending)
nitric oxide gas
sodium phenylbutyrate and taurursodiol
treprostinil SC
viltolarsen
albuterol/ipratropium
budesonide inhaled
budesonide rectal
palovarotene
sodium sulfate/potassium chloride/magnesium sulfate/polyethylene glycol
amino acids mixture
aminobenzoate potassium
elivaldogene autotemcel
naproxen and sumatriptan
sumatriptan intranasal
alglucerase
metformin/rosiglitazone
ertugliflozin/metformin
elosulfase alfa
calcium carbonate/magnesium hydroxide
starch suppository
abicipar pegol (FDA Approval Pending)
riboflavin 5′-phosphate ophthalmic
povidone ophthalmic
glycerin oropharyngeal
dimethicone topical
menthol topical, dimethicone topical
pramoxine topical, menthol topical and dimethicone topical
phosphorated carbohydrate
brilliant blue G ophthalmic
brolucizumab intravitreal
purified water, ophthalmic
hydroxyethyl cellulose ophthalmic
ranibizumab intravitreal implant
sodium chloride hypertonic, ophthalmic 
cetirizine ophthalmic
phentolamine ophthalmic
ganciclovir ophthalmic
triamcinolone intravitreal
ocriplasmin intravitreal
atoltivimab/maftivimab/odesivimab
pegcetacoplan intravitreal
triamcinolone acetonide extended-release injectable suspension
tobramycin/loteprednol ophthalmic
2-octyl cyanoacrylate
vitamins A & D topical
diphenhydramine/allantoin topical
pyrethrins/piperonyl butoxide
lodoxamide ophthalmic
obeticholic acid
fluocinolone intravitreal implant
sincalide
linaclotide
nedocromil ophthalmic
cysteamine ophthalmic
avacincaptad pegol intravitreal
azelastine ophthalmic
bacitracin ophthalmic
propylene glycol ophthalmic
rimexolone ophthalmic
metoclopramide intranasal
mirikizumab
netarsudil ophthalmic
cenegermin
dexamethasone ophthalmic insert
prednisolone ophthalmic
phenylephrine and cocoa butter rectal
phenylephrine and witch hazel topical
phenylephrine, pramoxine, glycerin and petrolatum rectal
bisacodyl rectal
aluminum hydroxide/magnesium carbonate
aluminum hydroxide/magnesium hydroxide
hyoscyamine spray
methenamine/methylene blue/ hyoscyamine/ sodium phosphate monobasic/ phenyl salicylate
phenylephrine
chlorophyll
castor oil
cholic acid
phenol oropharyngeal
articaine/epinephrine
antithymocyte globulin equine
aluminum hydroxide/magnesium trisilicate
methenamine/hyoscyamine
hydrocortisone topical/pramoxine topical
sodium fluoride topical
mesna
C1 esterase inhibitor recombinant
menthol and pectin
menthol oropharyngeal
pectin oropharyngeal
gepirone
Goldenseal
polyethylene glycol and electrolytes
polyethylene glycol/electrolytes/sodium ascorbate/ascorbic acid
brompheniramine/pseudoephedrine/dextromethorphan
brompheniramine phenylephrine
acetaminophen/doxylamine/phenylephrine
doxylamine/acetaminophen/pseudoephedrine/dextromethorphan
acetaminophen/doxylamine/dextromethorphan
acetaminophen/doxylamine/dextromethorphan/phenylephrine
eslicarbazepine
fluticasone and salmeterol
codeine, acetaminophen, butalbital and caffeine
codeine, chlorpheniramine and phenylephrine
iodine
povidone iodine
butalbital/aspirin/caffeine/codeine
polyethylene glycol 400/propylene glycol ophthalmic 
pegvaliase
amivantamab
iopamidol
codeine and pseudoephedrine
emtricitabine, rilpivirine, tenofovir DF
penicillin G aqueous
miconazole topical
miconazole vaginal
ciprofloxacin inhaled (Pending FDA approval)
ceftazidime/avibactam
ceftolozane/tazobactam
aztreonam inhalation
amphotericin B cholesteryl sulfate
miconazole oral
elvitegravir/cobicistat/emtricitabine/tenofovir DF
isavuconazonium sulfate
dapivirine intravaginal (FDA Approval Pending)
lamivudine/raltegravir
codeine/triprolidine/pseudoephedrine
cadexomer iodine
brompheniramine/pseudoephedrine
codeine/acetaminophen
codeine/guaifenesin
beclomethasone inhaled
epoetin beta/methoxy polyethylene glycol
voreloxin(Orphan Drug)
rociletinib
pitcher plant
phosphatidylserine
telotristat ethyl
copper CU 64 dotatate
urea topical
exenatide subdermal implant
asenapine transdermal
ethiodized oil
urea oral
miglustat
acalisib(Investigational)
acetophenazine
guggul
aceneuramic acid
mestranol/norethindrone
reishi
lactitol
vonoprazan fumarate
motherwort
silver nitrate
salicylic acid/sulfur shampoo
salicylic acid topical
ketorolac ophthalmic
ketoconazole topical
Japanese encephalitis virus vaccine
dibucaine topical ointment
ketorolac intranasal
ketorolac/phenylephrine ophthalmic
rotavirus oral vaccine, live
guarana
hops
krill oil
salicylic acid/coal tar shampoo
sufentanil SL
pancrelipase
passion flower
pepdite one plus
nivolumab and relatlimab
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tolvaptan +

may enhance the serum concentration when combined with tolvaptan

may enhance the serum concentration when combined with tolvaptan

curcumin

may enhance the serum concentration when combined with tolvaptan

may enhance the serum concentration when combined with tolvaptan

may enhance the serum concentration when combined with tolvaptan

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

citalopram

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

efavirenz

tolvaptan: they may enhance the serum concentration of CYP3A Inhibitors

primidone

may diminish the serum concentration when combined with tolvaptan

may diminish the serum concentration when combined with tolvaptan

isoniazid

may diminish the serum concentration when combined with tolvaptan

propofol

may diminish the serum concentration when combined with tolvaptan

selexipag

may diminish the serum concentration when combined with tolvaptan

desmopressin

may decrease the therapeutic effect when combined with desmopressin

sodium chloride

may increase the adverse effect when combined with tolvaptan

grapefruit

It may enhance the effect when combined with grapefruit by CYP3A4 metabolism

griseofulvin

It may diminish the effect when combined with griseofulvin by CYP3A4 metabolism

miconazole vaginal

It may enhance the effect when combined with miconazole vaginal by affecting CYP3A4 metabolism

enzalutamide

CYP3A strong enhancers of the small intestine may reduce the bioavailability of tolvaptan

nirmatelvir/ritonavir

may enhance the serum concentration of CYP3A4 inhibitors

sodium chloride nasal

sodium chloride increases the toxicity of tolvaptan

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

losartan

may increase the hyperkalemic effect when combined with angiotensin II receptor blockers

may increase the hyperkalemic effect when combined with ace inhibitors

quinapril

may increase the hyperkalemic effect when combined with ace inhibitors

ramipril

may increase the hyperkalemic effect when combined with ace inhibitors

rescinnamine

may increase the hyperkalemic effect when combined with ace inhibitors

spirapril

may increase the hyperkalemic effect when combined with ace inhibitors

may diminish the serum concentration when combined with tolvaptan

efavirenz

may diminish the serum concentration when combined with tolvaptan

digoxin

may enhance the serum concentration when combined with digoxin

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

amiloride

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

may increase the hyperkalemic effect when combined with potassium-sparing diuretics

dexamethasone

It may enhance the metabolism when combined with dexamethasone

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

losartan

may enhance the hyperkalemic effect

cilazapril

may enhance the hyperkalemic effect

enalapril

may enhance the hyperkalemic effect

enalaprilat

may enhance the hyperkalemic effect

lisinopril

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

amiloride

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

may enhance the hyperkalemic effect

paclitaxel

when both drugs are combined, there may be a high metabolism of tolvaptan 

lorlatinib

the effect of tolvaptan is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism

carvedilol

it enhances the serum potassium levels

telmisartan

it may enhance the serum potassium levels

primidone

may decrease the serum concentration

may decrease the serum concentration

may decrease the serum concentration

efavirenz

may decrease the serum concentration

isoniazid

may decrease the serum concentration

may decrease the serum concentration

donepezil transdermal

may decrease the serum concentration

efavirenz

may decrease the serum concentration

prednisolone

may decrease the serum concentration

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

isoniazid

may increase the serum concentration

mexiletine

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

curcumin

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

may increase the serum concentration

diacerein

may increase the serum concentration

may increase the serum concentration

tranylcypromine

may increase the serum concentration

phosphoric acid

the efficacy of phosphoric acid may be decreased due to an increase in rate of excretion

Actions and spectrum:

The actions of tolvaptan include:

Inhibiting the action of vasopressin: Tolvaptan blocks the activity of vasopressin, which reduces the amount of water reabsorbed by the kidneys and increases urine output.
Increasing urine output: By reducing water reabsorption in the kidneys, tolvaptan increases urine output, which helps to eliminate excess water from the body and restore normal levels of Na in the blood.
Restoring normal Na levels: By increasing urine output and reducing water retention, tolvaptan helps to restore normal levels of Na in the blood.

The spectrum of tolvaptan includes:

Hyponatremia: tolvaptan is used to treat hyponatremia, which is a condition where the level of Na in the blood is too low.
Heart failure: tolvaptan may be used in the management of heart failure, as it can help to reduce fluid retention and improve symptoms.
Polycystic kidney disease: tolvaptan is also approved for the treatment of polycystic kidney disease, a genetic disorder that causes cysts to form in the kidneys and can lead to kidney failure. It may help to slow the progression of the disease and improve kidney function.

Frequency defined

>10%

Samsca

Pollakiuria (4-11%)
Urinary output increased (11%)
Dry mouth (13%)
Thirst (16%)
Nausea (21%)

Jynarque

Dizziness (11.3%)
Diarrhea (13.3%)
Fatigue (13.6%)
Dry mouth (16%)
Thirst (63.7%)
Increased urination (69.5%)

1-10%

Samsca

Pyrexia (4%)
Anorexia (4%)
Hyperglycemia (6%)
Constipation (7%)
Weakness (9%)
GI bleeding (10%)

Jynarque

Palpitations (3.5%)
Hyperuricemia (3.9%)
Rash (4.2%)
Dry skin (4.9%)
Abdominal distension (4.9%)
Decreased appetite (7.2%)
Dyspepsia (7.9%)

Post marketing Reports

Investigations: Hypernatremia

Hepatobiliary disorders: Liver failure

Neurologic: Osmotic demyelination syndrome

Immune system disorders: anaphylactic shock and rash

Black Box Warning:

Contraindication/Caution:

Contraindication:

Known hypersensitivity: tolvaptan should not be used in patients who have a known hypersensitivity to tolvaptan or any of its components.
Severe liver impairment: tolvaptan is contraindicated in patients with severe liver impairment, such as those with cirrhosis or a Child-Pugh score greater than or equal to 10.
Concomitant use with strong CYP3A inhibitors: tolvaptan is contraindicated in patients taking strong inhibitors of the enzyme CYP3A, such as ketoconazole, itraconazole, clarithromycin, ritonavir, and others, as these drugs can increase tolvaptan blood levels and increase the risk of adverse effects.
Anuria: tolvaptan should not be used in patients who are unable to produce urine (anuria).
Hypovolemic hyponatremia: tolvaptan is not recommended for the treatment of hypovolemic hyponatremia, which is a type of hyponatremia caused by fluid loss.
Pregnancy: tolvaptan is classified as a pregnancy category C medication, meaning that it may be harmful to a developing fetus and should be used with caution during pregnancy.
Breastfeeding: tolvaptan is not recommended for use in breastfeeding mothers, as it may be excreted in breast milk and could potentially harm a nursing infant.

Caution:

Moderate liver impairment: tolvaptan should be used with caution in patients with moderate liver impairment, such as those with a Child-Pugh score of 7-9.
Concomitant use with CYP3A inducers: tolvaptan should be used with caution in patients taking drugs that induce the enzyme CYP3A, such as rifampin, carbamazepine, phenytoin, and others, as these drugs can decrease tolvaptan blood levels and reduce its effectiveness.
Dehydration: tolvaptan may increase urine output, which can lead to dehydration.
Hyperkalemia: tolvaptan can increase serum potassium levels, particularly in patients with underlying kidney disease. Patients should be monitored for hyperkalemia, and the dose of tolvaptan may need to be adjusted accordingly.
Hypotension: tolvaptan can cause a decrease in blood pressure, particularly in patients with underlying heart disease or taking medications that lower blood pressure. Patients should be monitored for hypotension, and the dose of tolvaptan may need to be adjusted accordingly.
Elderly patients: Elderly patients may be more sensitive to the effects of tolvaptan and may be at increased risk of adverse effects.
Hyponatremia due to SIADH: tolvaptan may be less effective in treating hyponatremia caused by the syndrome of inappropriate antidiuretic hormone secretion (SIADH).

Comorbidities:

Heart failure: tolvaptan may be used in patients with heart failure and hyponatremia.
Liver cirrhosis: Hyponatremia is a common complication of liver cirrhosis, and tolvaptan may be used to treat this condition. However, tolvaptan is contraindicated in patients with severe liver impairment.
Syndrome of inappropriate antidiuretic hormone secretion (SIADH): tolvaptan may be used to treat hyponatremia caused by SIADH, although it may be less effective in this condition.
Cancer: Some types of cancer, particularly lung cancer, can cause hyponatremia. tolvaptan may be used in these patients, although it is not approved specifically for this indication.
Central nervous system disorders: Certain conditions that affect the CNS, such as meningitis, encephalitis, or brain tumors, can cause hyponatremia. tolvaptan may be used to treat hyponatremia in these patients.

Pregnancy consideration: pregnancy category: not assigned

Lactation: It is not known whether tolvaptan is excreted in human milk.

Pregnancy category:

Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.
Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women.
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.
Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women.
Category N: There is no data available for the drug under this category.

Pharmacology:

Pharmacodynamics:

In patients with hyponatremia (low sodium levels in the blood), tolvaptan has been shown to increase serum sodium levels by promoting the excretion of excess water.

Pharmacokinetics:

Absorption

Distribution

tolvaptan is highly protein-bound (99%) and has a large volume of distribution, indicating that it is extensively distributed throughout the body.

Metabolism

Elimination and excretion

tolvaptan is primarily eliminated by renal excretion, with about 70% of a dose excreted unchanged in the urine. The remainder of the dose is eliminated in the feces (21%) and through metabolism (9%).

Administration:

tolvaptan should be taken with water, and food does not significantly affect its absorption.
The recommended starting dose of tolvaptan for the treatment of hyponatremia is typically 15 mg once daily. The dose can be increased to 30 mg once daily after at least 24 hours if the serum sodium concentration does not increase by at least 4 mEq/L or if symptoms of hyponatremia persist.
The maximum recommended daily dose of tolvaptan is 60 mg.
tolvaptan should be taken at the same time each day to maintain consistent drug levels in the blood.
tolvaptan should not be crushed or chewed, and the tablets should be swallowed whole.
tolvaptan may interact with other medications, so patients should inform their healthcare provider of all medications they are taking, including over the counter and herbal supplements.
Patients should be monitored regularly for changes in serum sodium concentration and for signs of liver dysfunction, especially during the first 18 days of treatment, as tolvaptan has been associated with an increased risk of hepatotoxicity.
tolvaptan should be discontinued if there is evidence of liver injury or if the serum alanine aminotransferase (ALT) level increases to three times the upper limit of normal.

Patient information leaflet

Generic Name: tolvaptan

Pronounced: [ tol-VAP-tan]

Why do we use tolvaptan?

Hyponatremia: tolvaptan is FDA-approved for the treatment of euvolemic or hypervolemic hyponatremia associated with cirrhosis, heart failure, and the syndrome of antidiuretic hormone secretion (SIADH). It works by increasing the excretion of free water and reducing water retention, leading to an increase in serum sodium levels.
Autosomal dominant polycystic kidney disease (ADPKD): tolvaptan has also been approved for the treatment of ADPKD, which is a genetic disorder characterized by the growth of numerous cysts in the kidneys. tolvaptan has been shown to slow the progression of kidney disease in patients with ADPKD by reducing the growth of kidney cysts.
Ascites: tolvaptan may be used off-label for the treatment of ascites, which is the accumulation of fluid in the abdominal cavity that can occur in patients with liver cirrhosis. tolvaptan can reduce fluid accumulation and improve symptoms in some patients with ascites.
Heart failure: tolvaptan has been investigated for its potential use in the treatment of acute decompensated heart failure, but its use in this context is not yet FDA-approved.

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