Papaverine (HCl)
Papaverine (HCl) is alkaloid devoid of narcotic properties and was first described and extracted from opium in 1848 and later synthesized in 1990. Papaverine (HCl) is a hydrochloride salt of opium alkaloid that may be obtained from opium after separation of morphine or prepared synthetically. Chemically Papaverine (HCl) is 6, 7-dimethoxy-1-veratrylisoquinoline. Papaverine (HCl) is a smooth muscle relaxant, dilates the arteries and increase the blood flow to the obstructed region, especially in the treatment of cerebral and the peripheral ischemia associated with arterial spasm and myocardial ischemia complicated by arrhythmias. Papaverine (HCl) is administered orally, intravenously and intramuscularly.
Primary Characteristics
It is of Natural origin and belongs to Alkaloid.
It belongs to Phosphodiesterase inhibitor pharmacological group on the basis of mechanism of action and also classified in Vasodilators pharmacological group. It is also classified under Calcium Channel Blocker .
Molecular Weight: 375.9 · pKa: 6.4 · Solubility in Water: 1 in 40 · Solubility in Alcohol: 1 in 120 · Non-proprietary name: Papaverine (HCl).
Pharmacokinetics
Absorption: Papaverine (HCl) has an oral bioavailability is 94% (±4%), pre-systemic (first-pass) metabolism accounts for 70%.
Distribution: Papaverine (HCl) has a volume of distribution is 0.99 - 1.52 l/kg. plasma protein binding is 87 %.
Elimination: it is metabolised via Hepatic, plasma half-life is 1.5 - 2.2 hr, renal excretion is > 50 %.
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Indications
Papaverine (HCl) is primarily indicated in conditions like Bronchospasm, Cerebral ischaemia, Cerebrovascular disease, Myocardial ischaemia, Pulmonary embolism, Smooth muscle spasm.
Contraindications
Papaverine (HCl) is contraindicated in conditions like Glucoma, Myocardial infarction, Cardiac failure, Cardiac stroke, Heart block, Bradycardia, Liver diseases.
Dosage
Papaverine (HCl)'s dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 75 mg | 75 mg | — | IV,IM,Intra Arterial | 1-2 min. every 3 hrs. |
| 187.5 mg | 187.5 mg | Every 8h | PO | |
| Paediatric Dosage (20kg) | ||||
| 0 – 0 | — | — | Safety not establushed | |
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Papaverine (HCl) in overdosage may give rise to further complications which include Jaundice , Precipitation of glaucoma .
Papaverine (HCl) is known to cause more or less tolerable side effects which are usually transient. These include Blurred vision, Drowsiness, Weakness.
Warnings / Precautions
Available Brands
None recorded.
Storage Conditions
Drug Classification
- 1.17.5 — Antispasmodics