- March 15, 2022
- Newsletter
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Brand Name :
Staxyn ODT, Levitra
Synonyms :
vardenafil, vardenafilo, vardenafilum
Class :
Phosphodiesterase-5 Enzyme Inhibitors
Dosage forms & Strengths
Film-coated tablet
2.5mg
5mg
10mg
20mg
10 mg orally, one-hour prior sexual activity
It may decrease to 5 mg or may increase to 20 mg
Based on effectiveness and tolerance, do not exceed more than 1 dose per day
Co-administration with CYP3A4 inhibitors
200 mg/day ketoconazole or 200 mg/day itraconazole
Dose of vardenafil should not exceed 5 mg/day
400 mg/day ketoconazole or 400 mg/day itraconazole
Dose of vardenafil should not exceed 2.5 mg/day
When combined with saquinavir, indinavir, clarithromycin, and atazanavir; do not exceed the dose of vardenafil more than 2.5 mg/72 hours
When combined with 500:
10 mg orally, one-hour prior sexual activity
It may decrease to 5 mg or may increase to 20 mg
Based on effectiveness and tolerance, do not exceed more than 1 dose per day
Dose Adjustments
In the case of hepatic impairment- Child-Pugh class B, 5 mg orally 1 hour before intimacy in the form of film coated tablet
Not recommended in Child-Pugh class C
For <65 years
A film-coated tablet 10 mg orally an hour before intimacy
May be decreased to 5 mg or increased to 20 mg, based on the efficacy and tolerance
Do not exceed more than 1 dose/day
10 mg orally disintegrating tablet is placed on the tongue an hour before intimacy
Do not exceed more than 1 dose/day
The medication is not interchangeable with 10 mg of the film-coated tablet
For >65 years
5 mg initial dose
As AUC and Cmax are higher in older adults as compared to young men
The drug is not indicated for pediatrics
Dosage forms & Strengths
Film-coated tablet
2.5mg
5mg
10mg
20mg
may enhance the serum concentration
May increase the vasodilatory effect when combined with Vasodilators
May increase the vasodilatory effect when combined with Vasodilators
amyl nitrite: they may increase the vasodilatory effect when combined with Phosphodiesterase 5 Inhibitors
may enhance the hypotensive effect of Alpha1-Blockers
bunazosin (Not available in the United States)
may enhance the hypotensive effect of Alpha1-Blockers
may enhance the hypotensive effect of Alpha1-Blockers
may enhance the hypotensive effect of Alpha1-Blockers
may enhance the hypotensive effect of Alpha1-Blockers
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may increase the vasodilatory effect
may increase the vasodilatory effect
may increase the vasodilatory effect
may increase the vasodilatory effect
may increase the vasodilatory effect
may increase the vasodilatory effect
may increase the vasodilatory effect
may increase the vasodilatory effect
Phosphodiesterase 5 Inhibitors: they may increase the hypotensive effect when combined with blood viscosity reducing agents
Phosphodiesterase 5 Inhibitors: they may increase the hypotensive effect when combined with blood viscosity reducing agents
both the drugs may enhance the risk of nephrotoxicity and ototoxicity
may enhance the effect of vasodilators
may enhance the effect of vasodilators
may enhance the effect of vasodilators
may enhance the effect of vasodilators
may enhance the effect of vasodilators
may increase the hypotensive effect of Blood Pressure Lowering Agents
may increase the hypotensive effect of Blood Pressure Lowering Agents
May enhances the effects of the other by pharmacodynamic synergism
Actions and Spectrum:
vardenafil is a medication used to treat erectile dysfunction (ED) in men. It belongs to a class of drugs known as phosphodiesterase type 5 (PDE5) inhibitors, which work by increasing blood flow to the penis, leading to improved erectile function.
The actions of vardenafil include:
The spectrum of vardenafil includes:
Frequency defined
>10%
Headache
Flushing
1-10%
Rhinitis
Dyspepsia
Flulike syndrome
Sinusitis
Back pain
Dizziness
Nausea
<1%
Anaphylaxis
Angina
Insomnia
Myocardial infarction
Postural hypotension
Priapism
Pruritus
Rash
The drug is contraindicated in patients hypersensitive to vardenafil.
Pregnancy consideration:
Category B
Breastfeeding warnings:
Excretion of vardenafil in breastmilk is unknown
Pregnancy category:
Pharmacology:
vardenafil is a medication that belongs to the class of drugs called phosphodiesterase type 5 (PDE5) inhibitors. It works by blocking the action of the enzyme PDE5, which usually breaks down cyclic guanosine monophosphate (cGMP) in the smooth muscle cells lining the blood vessels of the penis.
cGMP is a molecule that acts as a messenger, signaling the smooth muscle cells to relax, which allows blood to flow into the penis, leading to an erection. By blocking PDE5, vardenafil increases cGMP levels, improving blood flow to the penis and improving erectile function.
Pharmacodynamics:
The pharmacodynamics of vardenafil involves its ability to inhibit PDE5, which results in increased levels of cGMP and improved erectile function. vardenafil has more excellent selectivity for PDE5 than other PDE isoforms, reducing the likelihood of side effects.
Pharmacokinetics:
Absorption
The drug is rapidly absorbed
Bioavailability is 15%
The onset of action is 60 minutes
The peak plasma time is 30-120 min
Distribution
The protein-bound is 95%
The volume of distribution is 208L
Metabolism
The drug is metabolized in the liver by CYP2C9 and CYP3A4
The metabolites formed are M1
Elimination and Excretion
The half-life is 3-6 hours
The rate of total body clearance is 56 L/hr
The drug is excreted 95% in feces and 5% in urine
Administration:
vardenafil is a medication typically taken orally, about 30 to 60 minutes before sexual activity. The medication is in tablet form and should be taken with a full glass of water.
The recommended starting dose of vardenafil is 10 mg, although the dose may be adjusted based on individual response and tolerability. The maximum recommended dose is 20 mg per day.
vardenafil should not be taken more than once per day, and it should not be taken with grapefruit juice or high-fat meals, as these can affect the absorption and effectiveness of the medication.
Individuals taking vardenafil should avoid alcohol and not take the medication with other drugs that can interact with it, such as nitrates or nitric oxide donors.
Patient information leaflet
Generic Name: vardenafil
Pronounced: var-DEN-a-fil
Why do we use vardenafil?
vardenafil is used to treat erectile dysfunction (ED) in adult men. Erectile dysfunction is when a man has difficulty achieving or maintaining an erection sufficient for sexual activity. vardenafil works by increasing blood flow to the penis, which helps to improve erectile function. vardenafil belongs to a class of drugs called phosphodiesterase type 5 (PDE5) inhibitors, which also include sildenafil (Viagra) and tadalafil (Cialis).
These medications all work by inhibiting the action of the enzyme PDE5, which breaks down cyclic guanosine monophosphate (cGMP), a molecule that plays a role in erectile function. By blocking PDE5, vardenafil increases cGMP levels in the smooth muscle cells of the penis, leading to improved blood flow and better erectile function.