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papaverine

 
Dictionary: pa·pav·er·ine   (pə-păv'ə-rēn', -ər-ĭn) pronunciation
n.
A nonaddictive opium derivative, C20H21NO4, used medicinally to relieve spasms of smooth muscle.

[Latin papāver, poppy + -INE2.]


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Drug Info: Papaverine
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Brand names: Pavabid®, Pavacot®



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:
• an alcohol problem
• heart disease or irregular heartbeats
• liver disease
• glaucoma
• Parkinson's disease
• an unusual or allergic reaction to papaverine, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

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?

• alcohol
• barbiturate medicines for inducing sleep or treating seizures (convulsions)
• medicines for anxiety or sleeping problems, such as diazepam or temazepam
• medicines for Parkinson's disease
• some medicines for pain (narcotic analgesics such as morphine, tramadol)

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What 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:
• fainting or falling spells
• fast or irregular heartbeat
• stomach pain
• yellowing or the eyes or skin

Side effects that usually do not require medical attention report to your prescriber or health care professional if they continue or are bothersome):
• nausea or vomiting, decreased appetite, diarrhea, constipation
• dizziness
• drowsiness
• headache
• sweating or flushing

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store the bottle at room temperature at 15—30 degrees C (59—86 degrees F).


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.

 
Columbia Encyclopedia: papaverine
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papaverine (pəpăv'ərēn), alkaloid found in opium that acts as a muscle relaxant and vasodilator. The drug relaxes the smooth muscle of the larger blood vessels and is used to increase the blood supply to the brain or to the heart, as in the treatment of angina pectoris. It is also used in the treatment of some types of blood clot formation and in the treatment of impotence when the condition is caused by a lack of blood flow.


Veterinary Dictionary: papaverine
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An alkaloid obtained from opium and prepared synthetically; the hydrochloride salt is used as a smooth muscle relaxant.

Wikipedia: Papaverine
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Papaverine
Systematic (IUPAC) name
1-(3,4-dimethoxybenzyl)-6,7-dimethoxyisoquinoline
Identifiers
CAS number 58-74-2
61-25-6 (hydrochloride)
ATC code A03AD01 G04BE02
PubChem 4680
DrugBank APRD00628
Chemical data
Formula C20H21NO4 
Mol. mass 339.385 g/mol[1]
Pharmacokinetic data
Bioavailability 80%[3]
Protein binding ~90%
Metabolism Hepatic[3]
Half life 1.5–2 hours[3]
Excretion Renal[3]
Therapeutic considerations
Pregnancy cat.

USA: C[4]

Legal status
Routes Oral, intravenous, intramuscular, rectal,[5] intracavernosal

Papaverine (pronounced /pəˈpævəriːn/[1]) is an opium alkaloid 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 (opiates). In 1979, a Food and Drug Administration Advisory Committee evaluated studies on papaverine and concluded that there was a lack of objective data to support the therapeutic use of papaverine for these conditions. Papaverine remains available despite the committee's recommendation that it be withdrawn from the market.

Contents

Uses

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.

It is also commonly used in cryopreservation of blood vessels along with the other glycosaminoglycans and protein suspensions.[2][3] Functions as a vasodilator during cryopreservation when used in conjunction with verapamil, phentolamine, nifedipine, tolazoline or nitroprusside.[4][5]

Papaverine is also being investigated as a topical growth factor in tissue expansion with some success.[6]

Papaverine is also present in combinations of opium alkaloid salts such as Omnopon, Pantopon, Papaveretum, 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.

Mechanism

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.[7][8]

Side effects

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]

Formulations and trade names

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), Papaverin-Hamelin (Germany), Paveron (Germany), Spasmo-Nit (Germany),[5] Cardiospan, Papaversan, Cepaverin, Cerespan, Drapavel, Forpaven, Papalease, Pavatest, Paverolan, Therapav (France[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).

References

  1. ^ Papaverine - EverydayHealth.com[1]
  2. ^ E. Müller-Schweinitzer and P. Ellis: "Sucrose promotes the functional activity of blood vessels after cryopreservation in DMSO-containing fetal calf serum". Naunyn-Schmiedeberg's Archives of Pharmacology, Volume 345, Number 5 / May, 1992
  3. ^ Muller-Schweinitzer E, Hasse J, Swoboda L. : "Cryopreservation of human bronchi.". J Asthma. 1993;30(6):451-7. Links
  4. ^ Brockbank KG.: "Effects of cryopreservation upon vein function in vivo". Cryobiology. 1994 Feb;31(1):71-81
  5. ^ Joseph S. Giglia, Jeremy D. Ollerenshaw, Patti E. Dawson, Kirby S. Black, William M. Abbott: "Cryopreservation Prevents Arterial Allograft Dilation ". Annals of Vascular Surgery Volume 16, Number 6 / December, 2002
  6. ^ Tang Y, Luan J, Zhang X (2004). "Accelerating tissue expansion by application of topical papaverine cream". Plast. Reconstr. Surg. 114 (5): 1166–9. doi:10.1097/01.PRS.0000135854.48570.76. PMID 15457029. 
  7. ^ Siuciak JA, Chapin DS, Harms JF, Lebel LA, McCarthy SA, Chambers L, Shrikhande A, Wong S, Menniti FS, Schmidt CJ. Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis. Neuropharmacology. 2006 Aug;51(2):386-96. PMID 16780899
  8. ^ Hebb AL, Robertson HA, Denovan-Wright EM. Phosphodiesterase 10A inhibition is associated with locomotor and cognitive deficits and increased anxiety in mice. European Neuropsychopharmacology. 2008 May;18(5):339-63. PMID 17913473
  1. a  b  c  "SID 544606 -- PubChem Substance Summary". http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=544606. Retrieved 25 September 2005.  National Center for Biotechnology Information.
  2. a  "Papaverine Material Safety Data Sheet". http://bulkpharm.mallinckrodt.com/_attachments/msds/PAPVN.htm. Retrieved 25 September 2005. 
  3. a  b  c  d  e  f  g  h  Unknown (2000). "PAPAVERINE". Molécule(s) de base: PAPAVERINE. Biam. http://www.biam2.org/www/Sub3015.html. Retrieved 25 September 2005.  (French)
  4. a  Unknown (2004). "Who should not take papaverine?". papaverine Consumer Drug Information. Cerner Multum, Inc. http://www.drugs.com/MTM/papaverine.html. Retrieved 26 September 2005. 
  5. a  b  c  Unknown (1999). "PAPAVERINE CHLORHYDRATE". Molécule(s) de base: PAPAVERINE. Biam. http://www.biam2.org/www/Sub65.html. Retrieved 25 September 2005.  (French)
  6. a  Liu, James K.; Couldwell, William T (2005). "Intra-arterial papaverine infusions for the treatment of cerebral vasospasm induced by aneurysmal subarachnoid hemorrhage". Neurocritical Care 2 (2): 124–32. doi:10.1385/NCC:2:2:124. PMID 16159054.  Fulltext options List of Library Holdings
  7. a  Takeuchi K, Sakamoto S, Nagayoshi Y, Nishizawa H, Matsubara J (2004). "Reactivity of the human internal thoracic artery to vasodilators in coronary artery bypass grafting". European Journal of Cardio-Thoracic Surgery 26 (5): 956–9. doi:10.1016/j.ejcts.2004.07.047. PMID 15519189.  Fulltext options List of Library Holdings
  8. a  "SID 149219 -- PubChem Substance Summary". http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=149219. Retrieved 26 September 2005.  National Center for Biotechnology Information.
  9. a  Clyde BL, Firlik AD, Kaufmann AM, Spearman MP, Yonas H (1996). "Paradoxical aggravation of vasospasm with papaverine infusion following aneurysmal subarachnoid hemorrhage. Case report". Journal of Neurosurgery 84 (4): 690–5.  PubMed
  10. a  "Molécule de base: PAPAVERINE". http://www.biam2.org/www/Gsu1575.html. Retrieved 26 September 2005.  Biam.
  11. a  Unknown (1999). "PAPAVERINE TEPROSILATE". Molécule(s) de base: PAPAVERINE. Biam. http://www.biam2.org/www/Sub70.html. Retrieved 26 September 2005.  (French)
  12. a  Unknown (1998). "PAPAVERINE CODECARBOXYLATE". Molécule(s) de base: PAPAVERINE. Biam. http://www.biam2.org/www/Sub1293.html. Retrieved 26 September 2005.  (French)
  13. a  Unknown (1998). "PAPAVERINE ADENYLATE". Molécule(s) de base: PAPAVERINE. Biam. http://www.biam2.org/www/Sub1295.html. Retrieved 26 September 2005.  (French)
  14. a  "SID 660773 PubChem Substance Summary". http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=660773. Retrieved 25 September 2005.  National Center for Biotechnology Information.
  15. a  "SID 660767 -- PubChem Substance Summary". http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=660767. Retrieved 25 September 2005.  National Center for Biotechnology Information.
  16. a  "THERAPAV (PRODUIT PUR) - Détail". http://www.reptox.csst.qc.ca/Produit.asp?no_produit=108688&nom=THERAPAV+(PRODUIT+PUR)&incr=0. Retrieved 26 September 2005.  CSST - Service du répertoire toxicologique. (French)
  17. a  "SID 660767 -- PubChem Substance Summary - Depositor-Supplied Synonyms: All". http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=40460&ncount=61#Synonyms. Retrieved 26 September 2005.  National Center for Biotechnology Information.

 
 

 

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Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Columbia Encyclopedia. The Columbia Electronic Encyclopedia, Sixth Edition Copyright © 2003, Columbia University Press. Licensed from Columbia University Press. All rights reserved. www.cc.columbia.edu/cu/cup/ Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Papaverine" Read more