
[Latin papāver, poppy + -INE2.]
Brand names: Para-Time
Chemical formula:

Papaverine extended-release capsules
What are papaverine extended-release capsules?
PAPAVERINE (PAVABID®, PAVACOT®) is a vasodilator that relaxes blood vessels and makes them wider and allows the blood to pass through them more easily. Generic papaverine extended-release capsules are available.What should I tell my health care provider before I take this medicine?
They need to know if you have, or have had, any of these conditions:How should I use this medicine?
Take papaverine by mouth. Follow the directions on the prescription label. Swallow the capsules with a drink of water. Do not chew, open, break or crush the capsules. The capsules are formulated to release the drug slowly in your body. Take your doses at regular intervals. Do not take your medicine more often than directed.What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.What drug(s) may interact with papaverine?
alcoholWhat should I watch for while taking papaverine?
If you experience dizziness or feel faint, this may be due to the lowering of your blood pressure. Lie down immediately and raise your legs. If symptoms persist, call your prescriber or health care professional. Do not drive, use machinery, or do anything that requires mental alertness until you know how papaverine affects you.What side effects may I notice from using papaverine?
Side effects that you should report to your prescriber or health care professional as soon as possible:Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
| papaveretum, pantoprazole, panitumumab | |
| paracetamol, paraldehyde, parasympathetic nervous system |

| papain, pantoyl, pantothenyl | |
| paper chromatogram, paper chromatography, paper electrophoresis |
An alkaloid obtained from opium and prepared synthetically; the hydrochloride salt is used as a smooth muscle relaxant.
| Systematic (IUPAC) name | |
|---|---|
| 1-(3,4-dimethoxybenzyl)-6,7-dimethoxyisoquinoline | |
| Clinical data | |
| Trade names | Pavabid |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a682707 |
| Pregnancy cat. | USA: C[4] |
| Legal status | ? |
| Routes | Oral, intravenous, intramuscular, rectal,[5] intracavernosal |
| Pharmacokinetic data | |
| Bioavailability | 80%[3] |
| Protein binding | ~90% |
| Metabolism | Hepatic[3] |
| Half-life | 1.5–2 hours[3] |
| Excretion | Renal[3] |
| Identifiers | |
| CAS number | 58-74-2 61-25-6 (hydrochloride) |
| ATC code | A03AD01 G04BE02 |
| PubChem | CID 4680 |
| DrugBank | DB01113 |
| ChemSpider | 4518 |
| UNII | DAA13NKG2Q |
| KEGG | D07425 |
| ChEMBL | CHEMBL19224 |
| Chemical data | |
| Formula | C20H21NO4 |
| Mol. mass | 339.385 g/mol[1] |
| SMILES | eMolecules & PubChem |
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Papaverine (
/pəˈpævəriːn/)[1] is an opium alkaloid antispasmodic drug, used primarily in the treatment of visceral spasm, vasospasm (especially those involving the heart and the brain), and occasionally in the treatment of erectile dysfunction.[3] While it is found in the opium poppy, papaverine differs in both structure and pharmacological action from the analgesic (morphine-related) opium alkaloids (opioids).
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Papaverine was discovered in 1848 by Georg Merck (1825-1873).[2] Merck was a student of the German chemists Justus von Liebig and August Hofmann, and he was the son of Emanuel Merck (1794-1855), founder of the Merck corporation, a major German chemical and pharmaceutical company.[3]
Merck explained the origin of the name of "papaverine":
Original : " ... es ist mir gelungen, in einer in dem chemischen Laboratorium zu Giessen angestellten Untersuchung einiger in der Fabrik meines Vaters angehäuften Rückstände von Morphium-präparaten, eine neue Basis aufzufinden, welche ich mit dem Namen Papaverin bezeichnen werde."[4]
Translation : " ... while I was engaged at the Giessen chemical laboratory [of Justus von Liebig] in an investigation of some residues from morphine preparations, which had accumulated at my father's factory, I succeeded in discovering a new base, which I will designate with the name 'papaverin'."[5]
Papaverine is approved to treat spasms of the gastrointestinal tract, bile ducts and ureter and for use as a cerebral and coronary vasodilator[3] in subarachnoid hemorrhage (combined with balloon angioplasty)[6] and coronary artery bypass surgery.[7] Papaverine may also be used as a smooth muscle relaxant in microsurgery where it is applied directly to blood vessels.
Papaverine is used as an erectile dysfunction drug, alone or sometimes in combination.[6][7] Papaverine, when injected in penile tissue causes direct smooth muscle relaxation and consequent filling of the corpus cavernosum with blood resulting in erection. A topical gel is also available for ED treatment.[8]
It is also commonly used in cryopreservation of blood vessels along with the other glycosaminoglycans and protein suspensions.[9][10] Functions as a vasodilator during cryopreservation when used in conjunction with verapamil, phentolamine, nifedipine, tolazoline or nitroprusside.[11][12]
Papaverine is also being investigated as a topical growth factor in tissue expansion with some success.[13]
Papaverine is used as an off label prophylaxis (preventative) of migraine headaches.[14][15][16] It is not a first line drug such as a few beta blockers, calcium channel blockers, tricyclic antidepressants, and some anticonvulsants such as divalproex, but rather when these first line drugs and secondary drugs such as SSRIs, angiotensin II receptor antagonists, etc. fail in the prophylaxis of migraines, have intolerable side effects or are contraindicated.
Papaverine is also present in combinations of opium alkaloid salts such as papaveretum (Omnopon, Pantopon) and others, along with morphine, codeine, and in some cases noscapine and others in a percentage similar to that in opium, or modified for a given application.
The in vivo mechanism of action is not entirely clear, but an inhibition of the enzyme phosphodiesterase causing elevation of cyclic AMP levels is significant. It may also alter mitochondrial respiration.
Papaverine has also been demonstrated to be a selective phosphodiesterase inhibitor for the PDE10A subtype found mainly in the striatum of the brain. When administered chronically to mice, it produced motor and cognitive deficits and increased anxiety, but conversely may produce an antipsychotic effect.,[17][18] even though not all studies support this view.[19]
Frequent side effects of papaverine treatment include polymorphic ventricular tachycardia, constipation, interference with sulphobromophthalein[8] retention test (used to determine hepatic function), increased transaminase levels, increased alkaline phosphatase levels, somnolence, and vertigo.[3]
Rare side effects include flushing of the face, hyperhidrosis (excessive sweating), cutaneous eruption, arterial hypotension, tachycardia, loss of appetite, jaundice, eosinophilia, thrombopenia, mixed hepatitis, headache, allergic reaction, chronic active hepatitis,[3] and paradoxical aggravation of cerebral vasospasm.[9]
Papaverine is available as a conjugate of hydrochloride, codecarboxylate, adenylate, and teprosylate.[10] It was also once available as a salt of hydrobromide, camsylate, cromesilate, nicotinate, and phenylglycolate. The hydrochloride salt is available for intramuscular, intravenous, rectal and oral administration.[5] The teprosylate is available in intravenous, intramuscular, and orally administered formulations.[11] The codecarboxylate is available in oral form, only,[12] as is the adenylate.[13]
The codecarboxylate is sold under the name Albatran,[14] the adenylate as Dicertan,[15] and the hydrochloride salt is sold variously as Artegodan (Germany), Cardioverina (countries outside Europe and the United States), Dispamil (countries outside Europe and the United States), Opdensit (Germany), Panergon (Germany), Paverina Houde (Italy, Belgium), Pavacap (United States), Pavadyl (United States), Papaverine (Israel), Papaverin-Hamelin (Germany), Paveron (Germany), Spasmo-Nit (Germany),[5] Cardiospan, Papaversan, Cepaverin, Cerespan, Drapavel, Forpaven, Papalease, Pavatest, Paverolan, Therapav (Québec[16]), Vasospan, Cerebid, Delapav, Dilaves, Durapav, Dynovas, Optenyl, Pameion, Papacon, Pavabid, Pavacen, Pavakey, Pavased, Pavnell, Alapav, Myobid, Vasal, Pamelon, Pavadel, Pavagen, Ro-Papav, Vaso-Pav, Papanerin-hcl, Qua bid, Papital T.R., Paptial T.R., Pap-Kaps-150.[17]. In Hungary, papaverine and homatropine methylbromide are used in mild drugs that help "flush" the bile (e.g. Neo-Bilagit).
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