Papaverine: Difference between revisions

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{{drugbox
{{DrugProjectFormSinglePage
| IUPAC_name = 1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoquinoline
|authorTag=
| image = Papaverin - Papaverine.svg
 
| CAS_number = 61-25-6
 
| ATC_prefix = A03
<!--Overview-->
| ATC_suffix = AD01
 
| ATC_supplemental = {{ATC|G04|BE02}}
|genericName=
| PubChem = 4680
 
| DrugBank = APRD00628
 
| C=20 | H=21 | N=1 | O=4
 
| molecular_weight = 339.385 g/mol{{ref_label|1|1|c}}
|aOrAn=
| bioavailability = 80%{{ref_label|3|3|a}}
 
| protein_bound = ~90%
a
| metabolism = [[Hepatic]]{{ref_label|3|3|b}}
 
| elimination_half-life = 1.5–2 hours{{ref_label|3|3|c}}
|drugClass=
| pregnancy_category = [[United States|USA]]: C{{ref_label|4|4|a}}
 
| legal_status =  
 
| routes_of_administration = Oral, [[intravenous]], [[intramuscular]], rectal,{{ref_label|5|5|a}} [[intracavernosal]]
 
| excretion = [[Renal]]{{ref_label|3|3|d}}
|indication=
}}
 
{{SI}}
 
 
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* Dosing Information
 
:* Dosage
 
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* Dosing Information
 
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<!--Guideline-Supported Use (Adult)-->
 
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=====Condition1=====
 
* Developed by:
 
* Class of Recommendation:
 
* Strength of Evidence:
 
* Dosing Information
 
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<!--Non–Guideline-Supported Use (Adult)-->
 
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=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
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<!--Pediatric Indications and Dosage-->
 
<!--FDA-Labeled Indications and Dosage (Pediatric)-->
 
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=====Condition1=====
 
* Dosing Information
 
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=====Cardiovascular=====
 
 
 
=====Digestive=====
 
 
 
=====Endocrine=====
 
 
 
=====Hematologic and Lymphatic=====
 
 
 
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=====Neurologic=====
 
 
 
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<!--Administration and Monitoring-->
 
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* Oral
 
* Intravenous
 
|monitoring=
 
There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.
 
* Description
 
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===Acute Overdose===
 
====Signs and Symptoms====
 
* Description
 
====Management====
 
* Description
 
===Chronic Overdose===
 
There is limited information regarding <i>Chronic Overdose</i> of {{PAGENAME}} in the drug label.
 
<!--Pharmacology-->
 
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*
 
: [[File:{{PAGENAME}}01.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
 
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<!--Precautions with Alcohol-->
 
|alcohol=
 
* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.


<!--Brand Names-->


'''Papaverine''' 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]].{{ref_label|3|3|e}} While it is found in the [[opium poppy]], papaverine differs in both structure and pharmacological action from the other opium alkaloids ([[opiates]]).
|brandNames=
== Uses ==
Papaverine is approved to treat spasms of the gastointestinal tract, [[bile duct]]s and [[ureter]] and for use as a [[cerebral]] and [[coronary]] [[vasodilator]]{{ref_label|3|3|f}} in [[subarachnoid hemorrhage]] (combined with [[balloon angioplasty]]){{ref_label|6|6|a}} and [[coronary artery bypass surgery]].{{ref_label|7|7|a}} Papaverine may also be used as a smooth muscle relaxant in [[microsurgery]] where it is applied directly to blood vessels.


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 [[mitochondria]]l [[Cellular respiration|respiration]].
* ®<ref>{{Cite web | title = | url =  }}</ref>


It is also commonly used in [[cryopreservation]] of [[blood vessels]] along with other glycosaminoglycans and protein suspensions.<ref>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</ref><ref>Muller-Schweinitzer E, Hasse J, Swoboda L. : "Cryopreservation of human bronchi.". J Asthma. 1993;30(6):451-7. Links
<!--Look-Alike Drug Names-->
</ref> Functions as a [[vasodilator]] during cryopreservation when used in conjunction with [[verapamil]], [[phentolamine]], [[nifedipine]], tolazolines, or [[nitroprusside]].<ref>Brockbank KG.: "Effects of cryopreservation upon vein function in vivo". Cryobiology. 1994 Feb;31(1):71-81</ref><ref>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</ref>


Papaverine is also being investigated as a topical growth factor in tissue expansion with some success.<ref>{{cite journal |author=Tang Y, Luan J, Zhang X |title=Accelerating tissue expansion by application of topical papaverine cream |journal=Plast. Reconstr. Surg. |volume=114 |issue=5 |pages=1166–9 |year=2004 |pmid=15457029}}</ref>
|lookAlike=


== Side effects ==
* A® — B®<ref name="www.ismp.org">{{Cite web  | last =  | first =  | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>
Frequent side effects of papaverine treatment include polymorphic [[ventricular tachycardia]], constipation, interference with [[sulphobromophthalein]]{{ref_label|8|8|a}} [[retention test]] (used to determine hepatic function), increased [[transaminase]] levels, increased [[alkaline phosphatase]] levels, [[somnolence]], and [[Vertigo (medical)|vertigo]].{{ref_label|3|3|g}}


Rare side effects include flushing of the face, [[hyperhidrosis]] (excessive sweating), [[cutaneous eruption]], arterial [[hypotension]], tachycardia, lack of appetite, [[jaundice]], [[eosinophilia]], [[thrombopenia]], mixed [[hepatitis]], headache, allergic reaction, chronic active hepatitis,{{ref_label|3|3|h}} and paradoxical aggravation of cerebral vasospasm.{{ref_label|9|9|a}}
<!--Drug Shortage Status-->


== Formulations and trade names==
|drugShortage=
Papaverine is available as a [[Conjugated system|conjugate]] of [[hydrochloride]], [[pyridoxal phosphate|codecarboxylate]], [[adenosine monophosphate|adenylate]], and [[teprosylate]].{{ref_label|10|10|a}} It was also once available as a salt of [[hydrobromide]], [[camphorsulfonic acid|camsylate]], [[cromesilate]], [[nicotinic acid|nicotinate]], and [[amygdalic acid|phenylglycolate]]. The hydrochloride salt is available for intramuscular, intravenous, rectal and oral administration.{{ref_label|5|5|b}} The teprosylate is available in intravenous, intramuscular, and orally administered formulations.{{ref_label|11|11|a}} The codecarboxylate is available in oral form, only,{{ref_label|12|12|a}} as is the adenylate.{{ref_label|13|13|a}}
}}


The codecarboxylate is sold under the name Albatran®,{{ref_label|14|14|a}} the adenylate as Dicertan®,{{ref_label|15|15|a}} 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),{{ref_label|5|5|c}} Cardiospan®, Papaversan®, Cepaverin®, Cerespan®, Drapavel®, Forpaven®, Papalease®, Pavatest®, Paverolan®, Therapav® (France{{ref_label|16|16|a}}), 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®.{{ref_label|17|17|a}}
<!--Pill Image-->


==References==
{{PillImage
{{Reflist}}
|fileName=No image.jpg|This image is provided by the National Library of Medicine.
<div class="references-small">
|drugName=
# {{note_label|1|1|a}} {{note_label|1|1|b}} {{note_label|1|1|c}} {{cite web | url=http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=544606 | title=SID 544606 -- PubChem Substance Summary | accessdate=25 September | accessyear=2005 }} National Center for Biotechnology Information.
|NDC=
# {{note_label|2|2|a}} {{cite web | url=http://bulkpharm.mallinckrodt.com/_attachments/msds/PAPVN.htm | title=Papaverine Material Safety Data Sheet | accessdate=25 September | accessyear=2005 }}
|drugAuthor=
# {{note_label|3|3|a}} {{note_label|3|3|b}} {{note_label|3|3|c}} {{note_label|3|3|d}} {{note_label|3|3|e}} {{note_label|3|3|f}} {{note_label|3|3|g}} {{note_label|3|3|h}} {{cite web | | author=Unknown |
|ingredients=
year=2000 | title=PAPAVERINE | work=Molécule(s) de base : PAPAVERINE | publisher=Biam | url=http://www.biam2.org/www/Sub3015.html | accessdate=25 September | accessyear=2005}} (French)
|pillImprint=
# {{note_label|4|4|a}} {{cite web | author=Unknown | year=2004 | title=Who should not take papaverine? | work=papaverine Consumer Drug Information | publisher=Cerner Multum, Inc | url=http://www.drugs.com/MTM/papaverine.html | accessdate=26 September | accessyear=2005}}
|dosageValue=
# {{note_label|5|5|a}} {{note_label|5|5|b}} {{note_label|5|5|c}} {{cite web | author=Unknown |
|dosageUnit=
year=1999 | title=PAPAVERINE CHLORHYDRATE | work=Molécule(s) de base : PAPAVERINE | publisher=Biam | url=http://www.biam2.org/www/Sub65.html | accessdate=25 September | accessyear=2005}} (French)
|pillColor=
# {{note_label|6|6|a}} {{cite journal | author=Liu, James K.; Couldwell, William T | title=Intra-arterial papaverine infusions for the treatment of cerebral vasospasm induced by aneurysmal subarachnoid hemorrhage | journal=Neurocritical Care | volume=2 | issue=2 | year=2005 | pages=124-32 | id=PMID 16159054}} [http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&list_uids=16159054&dopt=ExternalLink Fulltext options] [http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&list_uids=16159054&dopt=ExternalLink&ExternalLink=libs List of Library Holdings]
|pillShape=
# {{note_label|7|7|a}} {{cite journal | author=Takeuchi K, Sakamoto S, Nagayoshi Y, Nishizawa H, Matsubara J | title=Reactivity of the human internal thoracic artery to vasodilators in coronary artery bypass grafting | journal=European Journal of Cardio-Thoracic Surgery | volume=26 | issue=5 | year=2004 | pages=956-9 | id=PMID 15519189}} [http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&list_uids=15519189&dopt=ExternalLink Fulltext options] [http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&list_uids=15519189&dopt=ExternalLink&ExternalLink=libs List of Library Holdings]
|pillSize=
# {{note_label|8|8|a}} {{cite web | url=http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=149219 | title=SID 149219 -- PubChem Substance Summary | accessdate=26 September | accessyear=2005 }} National Center for Biotechnology Information.
|pillScore=
# {{note_label|9|9|a}} {{cite journal | author=Clyde BL, Firlik AD, Kaufmann AM, Spearman MP, Yonas H | title=Paradoxical aggravation of vasospasm with papaverine infusion following aneurysmal subarachnoid hemorrhage. Case report | journal=Journal of Neurosurgery | volume=84 | issue=4 | year=1996 | pages=690-5}} {{PMID|8613866}}
}}
# {{note_label|10|10|a}} {{cite web | url=http://www.biam2.org/www/Gsu1575.html | title=Molécule de base : PAPAVERINE | accessdate=26 September | accessyear=2005 }} ''Biam.''
# {{note_label|11|11|a}} {{cite web | author=Unknown |
year=1999 | title=PAPAVERINE TEPROSILATE | work=Molécule(s) de base : PAPAVERINE | publisher=Biam | url=http://www.biam2.org/www/Sub70.html | accessdate=26 September | accessyear=2005}} (French)
# {{note_label|12|12|a}} {{cite web | author=Unknown | year=1998 | title=PAPAVERINE CODECARBOXYLATE | work=Molécule(s) de base : PAPAVERINE | publisher=Biam | url=http://www.biam2.org/www/Sub1293.html | accessdate=26 September | accessyear=2005}} (French)
# {{note_label|13|13|a}} {{cite web | author=Unknown | year=1998 | title=PAPAVERINE ADENYLATE | work=Molécule(s) de base : PAPAVERINE | publisher=Biam | url=http://www.biam2.org/www/Sub1295.html | accessdate=26 September | accessyear=2005}} (French)
# {{note_label|14|14|a}} {{cite web | url=http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=660773 | title=SID 660773 PubChem Substance Summary | accessdate=25 September | accessyear=2005 }} National Center for Biotechnology Information.
# {{note_label|15|15|a}} {{cite web | url=http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=660767 | title=SID 660767 -- PubChem Substance Summary | accessdate=25 September | accessyear=2005 }} National Center for Biotechnology Information.
# {{note_label|16|16|a}} {{cite web | url=http://www.reptox.csst.qc.ca/Produit.asp?no_produit=108688&nom=THERAPAV+(PRODUIT+PUR)&incr=0 | title=THERAPAV (PRODUIT PUR) - Détail | accessdate=26 September | accessyear=2005 }} CSST - Service du répertoire toxicologique. (French)
# {{note_label|17|17|a}} {{cite web | url=http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=40460&ncount=61#Synonyms | title=SID 660767 -- PubChem Substance Summary - Depositor-Supplied Synonyms: All | accessdate=26 September | accessyear=2005 }} National Center for Biotechnology Information.
</div>


{{Drugs for functional gastrointestinal disorders}}
<!--Label Display Image-->
{{Urologicals}}


{{LabelImage
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
}}


[[Category:Natural opium alkaloids]]
{{LabelImage
[[Category:Vasodilators]]
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
[[Category:Drugs]]
}}


[[pl:Papaweryna]]
<!--Category-->
[[de:Papaverin]]
[[eo:Papaverino]]
[[fr:Papavérine]]
[[ja:パパベリン]]
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[[sk:Papaverín]]
[[sv:Papaverin]]


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Revision as of 20:02, 16 January 2015

Papaverine
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1];

Disclaimer

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Black Box Warning

Title
See full prescribing information for complete Boxed Warning.
ConditionName:
  • Content

Overview

Papaverine is a that is FDA approved for the {{{indicationType}}} of . There is a Black Box Warning for this drug as shown here. Common adverse reactions include .

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Condition1
  • Dosing Information
  • Dosage
Condition2
  • Dosing Information
  • Dosage
Condition3
  • Dosing Information
  • Dosage
Condition4
  • Dosing Information
  • Dosage

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Papaverine in adult patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Papaverine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding FDA-Labeled Use of Papaverine in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Papaverine in pediatric patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Papaverine in pediatric patients.

Contraindications

  • Condition1

Warnings

Title
See full prescribing information for complete Boxed Warning.
ConditionName:
  • Content
  • Description

Precautions

  • Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Papaverine in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Papaverine in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Drug Interactions

  • Drug
  • Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Papaverine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Papaverine during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Papaverine with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Papaverine with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Papaverine with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Papaverine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Papaverine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Papaverine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Papaverine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Papaverine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Papaverine in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral
  • Intravenous

Monitoring

There is limited information regarding Monitoring of Papaverine in the drug label.

  • Description

IV Compatibility

There is limited information regarding IV Compatibility of Papaverine in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Papaverine in the drug label.

Pharmacology

There is limited information regarding Papaverine Pharmacology in the drug label.

Mechanism of Action

Structure

File:Papaverine01.png
This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Papaverine in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Papaverine in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Papaverine in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Papaverine in the drug label.

How Supplied

Storage

There is limited information regarding Papaverine Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Papaverine in the drug label.

Precautions with Alcohol

  • Alcohol-Papaverine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. ↑ Empty citation (help)
  2. ↑ "http://www.ismp.org". External link in |title= (help)


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