argipressin

Action and Spectrum

Actions and Spectrum: 

Actions: 

Argipressin helps the body retain water. It works by making the kidney tubules absorb more water. Additionally, argipressin contracts smooth muscle in the gut and blood vessels. It affects capillaries, small arteries, and veins most strongly. Bigger veins are less affected. Notably, its effects on muscle contraction don’t need nerves. Argipressin acts directly, whether nerves are present or not. This shows its unique ability to impact both kidneys and blood vessels. 

Spectrum: 

Researchers noticed that cells called mononuclear phagocytes made more prostaglandin E2 (PGE2) when exposed to arginine vasopressin (AVP). They found that while DP, an AVP-like molecule, was less potent, it still boosted PGE2 production. Macrophages treated with indomethacin showed higher levels of cyclic AMP due to AVP. Interestingly, adding PGE2 to macrophage cultures didn’t change their ability to bind [3H]AVP. Bell and colleagues showed AVP can alter immunity by inducing the autologous mixed lymphocyte response. The arginine in position 8 of AVP increased lymphocyte proliferation. This heightened proliferation, combined with AVP receptors on blood and spleen cells, suggests AVP directly stimulates the immune system. Peptide-antagonists of AVP’s V1a, V1b, and V2 receptors further support this link between the neuroendocrine and immune systems by inhibiting AVP binding. In summary, laboratory studies definitively demonstrate AVP’s role in boosting immunity. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

Vertigo 

Throbbing headache 

Hypersensitivity reactions 

Pallor 

Abdominal cramps 

Anginal pain 

Desire to defaecate 

Gangrene 

Water intoxication 

Urticaria 

Myocardial infarction 

Flatulence 

Bronchoconstriction 

Constriction of coronary arteries 

Eructation 

Peripheral ischaemia 

Sweating 

Tremor 

Fluid retention 

Vomiting 

Myocardial ischaemia 

Anaphylaxis 

Black Box Warning

Black Box Warning: 

Exercise care when administering this drug to patients with vascular conditions, particularly coronary artery disease, and hypertension. High doses risk triggering a heart attack, while smaller amounts may induce discomfort. For those with peripheral vascular issues, closely observe their skin for potential ischemic signs. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• HTN 
• Chronic nephritis (until normalized blood nitrogen levels reached) 
• Vascular disorder 

Cautions 

• Renal impairment 
• Vascular disease (especially coronary artery disease) and systemic hypertension 
• Peripheral vascular disease 
• Epilepsy 
• Migraine 
• Asthma 
• Heart failure 
• Fluid intake considerations to avoid hyponatraemia and water intoxication 
• Monitoring for early signs of water intoxication 
• Potential vertigo, with caution regarding driving or operating machineryDrug interactions 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

Pregnancy category: B2 

Medicine treats diabetes insipidus in pregnancy safely, without harming the baby. During pregnancy’s last months and delivery, women have triple average vasopressin amounts compared to non-pregnant women.    Vasopressin shots or nasal sprays can cause uterine contractions because they’re like oxytocin. But you should try non-drug treatments first when pregnant if possible. If medicine’s needed, use the safest kind with proven safety and lowest helpful dose for the shortest time. Avoid mixing many medicines. Be extra careful with drugs that may cause birth defects, especially very early in pregnancy. However, if drug exposure happens in the first two weeks after conception, you may be reassured since those drugs clear the body quickly and you know the exact conception date. 

Breastfeeding warnings:  

Doctors have used argipressin for breastfeeding ladies without harm to their babies. But some situations need care – babies that are new, not fully grown yet, underweight, stomach problems, or very sick. If moms must take medicine, they should get the smallest amount for the least time. And if breastfeeding can’t be stopped, taking medicine right after feeding lowers the baby’s exposure. Watch babies on meds through breastmilk for odd signs or issues. Consider if the baby’s medications might impact the one from breastmilk. 

Pregnancy categories: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

<b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

Argipressin has an antidiuretic effect. This is due to it helping reabsorb water in the renal tubules. Additionally, it makes smooth muscles contract in the gastrointestinal tract and cardiovascular system parts. It especially affects capillaries, arterioles (small arteries), and venules (small veins). However, it does not affect more prominent veins much. Its direct impact on contractile elements is not stopped by adrenergic blocking agents or vascular denervation. This highlights argipressin’s distinct, direct physiological actions on renal and vascular processes. 

Arginine-vasopressin (AVP) is an essential antidiuretic hormone made by the posterior pituitary gland. It enters the bloodstream from the hypothalamus. AVP is known for its role in water retention and glucose regulation. It acts on various tissues through distinct receptor subtypes like V2R, V1aR, and V1bR. Its release, along with copeptin, is linked to obesity and insulin resistance: it can predict diabetes             development. In diabetes, high plasma AVP levels are seen, affecting glucagon and insulin secretion based on blood glucose levels. AVP, primarily from the hypothalamus, may also be produced in other body parts, potentially regulating islet hormone secretion. Experiments in rats show AVP injections dose-dependently increase blood glucose via gluconeogenic effects in the liver, mainly through V1aR. AVP analogs targeting V1aR and V1bR show promise for improving metabolic syndrome parameters in mice. However, effects seen in animal studies may differ in humans due to lower circulating AVP and oxytocin plasma levels. 

Pharmacodynamics: 

Researchers test vasopressin’s effects outside the body using established methods. They assess how analogs (alone or mixed with AVP) impact blood pressure (V1) or urine flow (V2). However, no reliable in vivo tests exist for vasopressin’s central nervous system effects. While binding assays study CNS peptide receptors (including AVP), a significant gap separates in vitro and in vivo receptor activation. Bridging this divide      requires developing bioassay models to combine insights from both experiment types. Specific criteria must be met to prove a physiological role for a neuropeptide. Recent reviews suggest vasopressin likely plays an essential physiological role in fever and antipyresis. 

Pharmacokinetics: 

Absorption 

Argipressin injection gets absorbed into the body when given under the skin or into the muscle. The medication then enters the bloodstream. Its ability to decrease urination lasts for a period ranging from 2 to 8 hours. 

Distribution 

Argipressin goes all over the body once it gets in the blood. Different organs and tissues take it in how the medicine spreads, which may change how long it controls peeing in each person. 

Metabolism 

The body changes most of the given dose, with the liver and kidneys playing a crucial role. These organs break down argipressin into smaller parts. The liver and kidneys help this drug gets destroyed quickly, which contributes to its overall change by the body. 

Elimination and Excretion 

Argipressin can be given through multiple routes: beneath the skin, into muscles, or veins. Further dilution must occur when used intravenously to treat enlarged veins in the {esophagus. The medication blends into a greater fluid volume, permitting dosing that is customized for each person’s requirements. Argipressin mixes well with 5% glucose solution and 0.9% sodium chloride injection. Therefore, convenience and versatility characterize its use in various medical situations. 

Adminstartion

Administration: 

Argipressin is a drug with many ways of giving it to patients. It works for shots under the skin, into muscle, or veins. When doctors use it in veins for problems like oesophageal varices, they must dilute it more in a larger liquid amount. This makes giving the correct dose for each patient’s needs possible. Argipressin mixes well with 5% glucose injections and 0.9% sodium chloride injections. This flexibility helps doctors use it easily in different situations. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: argipressin 

Pronounced: ahr-ji-PRES-in 

Why do we use argipressin? 

Argipressin has many uses. It’s helpful for diabetes insipidus symptoms like being thirsty and often urination. It makes your urine more concentrated. Argipressin also helps with heavy bleeding or shock by constricting blood vessels, raising blood pressure. It can work like epinephrine during cardiac arrest, improving blood flow in CPR. In some shock conditions and tests for excessive thirst or urination, argipressin plays a part, too. Healthcare    workers must carefully give argipressin, as wrong dosing can lead to complications.