Papaverine: Difference between revisions

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|drugClass=[[phosphodiesterase]] [[inhibitor]]
|drugClass=[[phosphodiesterase]] [[inhibitor]]
|indicationType=treatment
|indicationType=treatment
|indication=vascular spasm associated with acute [[myocardial infarction]] ([[coronary occlusion]]), [[angina pectoris]], [[peripheral vascular disease]],peripheral and [[pulmonary embolism]]
|indication=vascular spasm associated with acute [[myocardial infarction]] ([[coronary occlusion]]), [[angina pectoris]], [[peripheral vascular disease]], peripheral and [[pulmonary embolism]]
|adverseReactions=general discomfort, [[nausea]], [[abdominal discomfort]], [[anorexia]], [[skin rash]], [[malaise]], [[vertigo]] and [[headache]].
|adverseReactions=general discomfort, [[nausea]], [[abdominal discomfort]], [[anorexia]], [[skin rash]], [[malaise]], [[vertigo]] and [[headache]].
|blackBoxWarningTitle=Title
|blackBoxWarningTitle=Title
Line 15: Line 15:


<!--FDA-Labeled Indications and Dosage (Adult)-->
<!--FDA-Labeled Indications and Dosage (Adult)-->
|fdaLIADAdult=*Papaverine is recommended in various conditions accompanied by spasm of smooth muscle, such as vascular spasm associated with acute myocardial infarction (coronary occlusion), angina pectoris, peripheral and pulmonary embolism, peripheral vascular disease in which there is a vasospastic element, or certain cerebral angiospastic states; and visceral spasm, as in ureteral, biliary, or gastrointestinal colic.
|fdaLIADAdult=*Papaverine is recommended in various conditions accompanied by spasm of smooth muscle, such as vascular spasm associated with acute [[myocardial infarction]] ([[coronary occlusion]]), [[angina pectoris]], peripheral and [[pulmonary embolism]], [[peripheral vascular disease]] in which there is a vasospastic element, or certain cerebral angiospastic states; and visceral spasm, as in ureteral, biliary, or gastrointestinal [[colic]].
* Dosage
* Dosage
:*Papaverine Hydrochloride may be administered intravenously or intramuscularly. The intravenous route is recommended when an immediate effect is desired, but the drug must be injected slowly over the course of 1 or 2 minutes to avoid uncomfortable or alarming side effects.
:*Papaverine Hydrochloride may be administered intravenously or intramuscularly. The intravenous route is recommended when an immediate effect is desired, but the drug must be injected slowly over the course of 1 or 2 minutes to avoid uncomfortable or alarming side effects.


:*Parenteral administration of papaverine hydrochloride in doses of 1 to 4 mL is repeated every 3 hours as indicated. In the treatment of cardiac extrasystoles, 2 doses may be given 10 minutes apart.
:*Parenteral administration of papaverine hydrochloride in doses of 1 to 4 mL is repeated every 3 hours as indicated. In the treatment of [[cardiac extrasystoles]], 2 doses may be given 10 minutes apart.




Line 26: Line 26:


<!--Guideline-Supported Use (Adult)-->
<!--Guideline-Supported Use (Adult)-->
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Papaverine in adult patients.


<!--Non–Guideline-Supported Use (Adult)-->
<!--Non–Guideline-Supported Use (Adult)-->
Line 36: Line 36:


<!--Guideline-Supported Use (Pediatric)-->
<!--Guideline-Supported Use (Pediatric)-->
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Papaverine in pediatric patients.


<!--Non–Guideline-Supported Use (Pediatric)-->
<!--Non–Guideline-Supported Use (Pediatric)-->
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Papaverine in pediatric patients.
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Papaverine in pediatric patients.
|contraindications=* complete atrioventricular heart block
|contraindications======Complete atrioventricular heart block=====
:*Intravenous injection of papaverine is contraindicated in the presence of complete atrioventricular heart block. When conduction is depressed, the drug may produce transient ectopic rhythms of ventricular origin, either premature beats or paroxysmal tachycardia.
*Intravenous injection of papaverine is contraindicated in the presence of [[complete atrioventricular heart block]]. When conduction is depressed, the drug may produce transient [[ectopic rhythms]] of ventricular origin, either [[premature beats]] or [[paroxysmal tachycardia]].
 
=====Impotence=====
*Papaverine Hydrochloride is not indicated for the treatment of impotence by intracorporeal injection. The intracorporeal injection of papaverine hydrochloride has been reported to have resulted in persistent priapism requiring medical and surgical intervention.
*Papaverine Hydrochloride is not indicated for the treatment of [[impotence]] by [[intracorporeal injection]]. The [[intracorporeal injection]] of papaverine hydrochloride has been reported to have resulted in persistent [[priapism]] requiring medical and surgical intervention.


<!--Warnings-->
<!--Warnings-->
|warnings=* Description
|warnings=====Precautions====
 
====Precautions====


* Description
*Papaverine Hydrochloride Injection, USP, should not be added to Lactated Ringer’s Injection, because precipitation would result.


*Papaverine Hydrochloride should be used with caution in patients with glaucoma. The medication should be discontinued if hepatic [[hypersensitivity]] with gastrointestinal symptoms, [[jaundice]], or [[eosinophilia]] becomes evident or if [[liver function test]] values become altered.
*[[Drug dependence]] resulting from the abuse of many of the selective depressants, including papaverine hydrochloride, has been reported.
<!--Adverse Reactions-->
<!--Adverse Reactions-->


<!--Clinical Trials Experience-->
<!--Clinical Trials Experience-->
|clinicalTrials=There is limited information regarding <i>Clinical Trial Experience</i> of {{PAGENAME}} in the drug label.
|clinicalTrials=*The following side effects have been reported: general discomfort, [[nausea]], [[abdominal discomfort]], [[anorexia]], [[constipation]] or [[diarrhea]], [[skin rash]], [[malaise]], [[vertigo]], [[headache]], intensive [[flushing]] of the face, [[perspiration]], increase in the depth of respiration, increase in [[heart rate]], a slight rise in [[blood pressure]], and excessive [[sedation]].
 
=====Body as a Whole=====
 
 
 
 
=====Cardiovascular=====
 
 
 
 
=====Digestive=====
 
 
 
 
=====Endocrine=====
 
 
 
 
=====Hematologic and Lymphatic=====
 
 
 
 
=====Metabolic and Nutritional=====
 
 
 
 
=====Musculoskeletal=====
 
 
 
 
=====Neurologic=====
 
 
 
 
=====Respiratory=====
 
 
 
 
=====Skin and Hypersensitivy Reactions=====
 
 
 
 
=====Special Senses=====
 
 
 
 
=====Urogenital=====
 
 
 
 
=====Miscellaneous=====
 
 


*[[Hepatitis]], probably related to an immune mechanism, has been reported infrequently. Rarely, this has progressed to [[cirrhosis]].
<!--Postmarketing Experience-->
<!--Postmarketing Experience-->
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of Papaverine in the drug label.


=====Body as a Whole=====


<!--Drug Interactions-->
|FDAPregCat=C
|useInPregnancyFDA=*No teratogenic effects were observed in rats when papaverine hydrochloride was administered subcutaneously as a single agent. It is not known whether papaverine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. *Papaverine Hydrochloride should be given to a pregnant woman only if clearly needed.
|useInPregnancyAUS=There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Papaverine in women who are pregnant.
|useInLaborDelivery=There is no FDA guidance on use of Papaverine during labor and delivery.
|useInNursing=*It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when papaverine hydrochloride is administered to a nursing woman.
|useInPed=Safety and effectiveness in children have not been established.
|useInGeri=There is no FDA guidance on the use of Papaverine with respect to geriatric patients.
|useInGender=There is no FDA guidance on the use of Papaverine with respect to specific gender populations.
|useInRace=There is no FDA guidance on the use of Papaverine with respect to specific racial populations.
|useInRenalImpair=There is no FDA guidance on the use of Papaverine in patients with [[renal impairment]].
|useInHepaticImpair=There is no FDA guidance on the use of Papaverine in patients with hepatic impairment.
|useInReproPotential=There is no FDA guidance on the use of Papaverine in women of reproductive potentials and males.
|useInImmunocomp=There is no FDA guidance one the use of Papaverine in patients who are [[immunocompromised]].


<!--Administration and Monitoring-->
|administration=* Intravenously or Intramuscularly
|monitoring=There is limited information regarding <i>Monitoring</i> of Papaverine in the drug label.


=====Cardiovascular=====


<!--IV Compatibility-->
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of Papaverine in the drug label.


<!--Overdosage-->
|overdose======Signs and Symptoms=====
*The symptoms of toxicity from papaverine hydrochloride often result from vasomotor instability and include [[nausea]], [[vomiting]], [[weakness]], central nervous system depression, [[nystagmus]], [[diplopia]], [[diaphoresis]], [[flushing]], [[dizziness]], and [[sinus tachycardia]].
* In large overdoses, papaverine is a potent inhibitor of cellular respiration and a weak [[calcium antagonist]].
*Following an oral overdose of 15 g, [[metabolic acidosis]] with [[hyperventilation]], [[hyperglycemia]], and [[hypokalemia]] have been reported. No information on toxic serum concentrations is available.
*Following intravenous overdosing in animals, [[seizures]], [[tachyarrhythmias]], and [[ventricular fibrillation]] have been reported.  The oral median lethal dose in rats is 360 mg/kg.


=====Digestive=====
=====Management =====
*To obtain up-to-date information about the treatment of overdose, a good resource is your certified Regional Poison Control Center. In managing overdosage, consider the possibility of multiple drug overdoses, interaction among drugs, and unusual [[drug kinetics]] in your patient.
*No specific antidote is known.
*Treatment should be [[symptomatic and supportive]].
*Protect the patient’s airway and support [[ventilation]] and [[perfusion]]. Meticulously monitor vital signs, [[blood gases]], blood chemistry values, and other variables.


*If convulsions occur, consider [[diazepam]], [[phenytoin]], or [[phenobarbital]]. If the [[seizures]] are refractory, general [[anesthesia]] with [[thiopental]] or [[halothane]] and [[paralysis]] with a [[neuromuscular blocking agent]] may be necessary.


*For [[hypotension]], consider intravenous fluids, elevation of the legs, and an [[inotropic vasopressor]], such as [[dopamine]] or [[norepinephrine]] ([[levarterenol]]). Theoretically, [[calcium gluconate]] may be helpful in treating some of the toxic cardiovascular effects of papaverine; monitor the [[ECG]] and [[plasma calcium]] concentrations.


=====Endocrine=====
*Forced [[diuresis]], [[peritoneal dialysis]], [[hemodialysis]], or charcoal [[hemoperfusion]] have not been established as beneficial for an overdose of papaverine hydrochloride.
<!--Pharmacology-->


<!--Drug box 2-->
|drugBox=[[File:Papaverine 04.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
|mechAction=*The most characteristic effect of papaverine is relaxation of the tonus of all smooth muscle, especially when it has been spasmodically contracted. Papaverine Hydrochloride apparently acts directly on the muscle itself. This relaxation is noted in the vascular system and bronchial musculature and in the gastrointestinal, biliary and urinary tracts.


*The main actions of papaverine are exerted on cardiac and smooth muscle. Papaverine relaxes various [[smooth muscle]]s, especially those of larger [[arteries]]; this relaxation may be prominent if spasm exists. The antispasmodic effect is a direct one and unrelated to muscle innervation, and the muscle still responds to drugs and other stimuli causing contraction.  Papaverine has minimal actions on the central nervous system, although very large doses tend to produce some sedation and sleepiness in some patients. In certain circumstances, mild respiratory stimulation can be observed, but this is therapeutically inconsequential. Papaverine stimulates respiration by acting on carotid and aortic body [[chemoreceptor]]s.


=====Hematologic and Lymphatic=====
*Papaverine relaxes the smooth musculature of the larger blood vessels, including the coronary, cerebral, peripheral, and pulmonary arteries. This action is particularly evident when such vessels are in spasm, induced reflexly or by drugs, and it provides the basis for the clinical use of papaverine in peripheral or pulmonary [[arterial embolism]].


*Experimentally in dogs, the alkaloid has been shown to cause fairly marked and long-lasting coronary [[vasodilatation]] and an increase in coronary blood flow. However, it also appears to have a direct [[inotropic]] effect and, when increased mechanical activity coincides with decreased systemic pressure, increases in coronary blood flow may not be sufficient to prevent brief periods of hypoxic [[myocardial depression]].




=====Metabolic and Nutritional=====
<!--Structure-->
 
|structure=* Papaverine Hydrochloride, USP, is the hydrochloride of an alkaloid obtained from opium or prepared synthetically. It belongs to the [[benzylisoquinoline]] group of alkaloids. It does not contain a [[phenanthrene]] group as do [[morphine]] and [[codeine]].
 
 
=====Musculoskeletal=====
 


*Papaverine Hydrochloride, USP, is 6,7-dimethoxy-1- veratrylisoquinoline hydrochloride and contains, on the dried basis, not less than 98.5% of C20H21NO4•HCI. The molecular weight is 375.85. The structural formula is as shown.


=====Neurologic=====
[[File:Papaverine 01.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]


*Papaverine Hydrochloride occurs as white crystals or white [[crystalline powder]]. One gram dissolves in about 30 mL of water and in 120 mL of alcohol. It is soluble in chloroform and practically insoluble in ether.


*Papaverine Hydrochloride Injection, USP, is a clear, colorless to pale-yellow solution.


=====Respiratory=====
*Papaverine Hydrochloride, for parenteral administration, is a smooth-muscle relaxant that is available in vials containing 30 mg/mL. Each vial also contains edetate disodium 0.005%. The 10 mL vials also contain [[chlorobutanol]] 0.5% as a preservative. pH may be adjusted with [[sodium citrate]] and/or [[citric acid]].
 
 
 
=====Skin and Hypersensitivy Reactions=====
 
 
 
=====Special Senses=====
 
 
 
=====Urogenital=====
 
 
 
=====Miscellaneous=====
 
 
 
<!--Drug Interactions-->
|drugInteractions=* Drug
:* Description
 
<!--Use in Specific Populations-->
|useInPregnancyFDA=* '''Pregnancy Category'''
|useInPregnancyAUS=* '''Australian Drug Evaluation Committee (ADEC) Pregnancy Category'''
 
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of {{PAGENAME}} in women who are pregnant.
|useInLaborDelivery=There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
|useInNursing=There is no FDA guidance on the use of {{PAGENAME}} with respect to nursing mothers.
|useInPed=There is no FDA guidance on the use of {{PAGENAME}} with respect to pediatric patients.
|useInGeri=There is no FDA guidance on the use of {{PAGENAME}} with respect to geriatric patients.
|useInGender=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific gender populations.
|useInRace=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific racial populations.
|useInRenalImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with renal impairment.
|useInHepaticImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with hepatic impairment.
|useInReproPotential=There is no FDA guidance on the use of {{PAGENAME}} in women of reproductive potentials and males.
|useInImmunocomp=There is no FDA guidance one the use of {{PAGENAME}} in patients who are immunocompromised.
 
<!--Administration and Monitoring-->
|administration=* Oral
 
* Intravenous
|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.
 
* Description
 
<!--IV Compatibility-->
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.
 
<!--Overdosage-->
|overdose====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-->
 
<!--Drug box 2-->
|drugBox=<!--Mechanism of Action-->
|mechAction=*
 
<!--Structure-->
|structure=*
 
: [[File:{{PAGENAME}}01.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]


<!--Pharmacodynamics-->
<!--Pharmacodynamics-->
|PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.
|PD=There is limited information regarding <i>Pharmacodynamics</i> of Papaverine in the drug label.


<!--Pharmacokinetics-->
<!--Pharmacokinetics-->
|PK=There is limited information regarding <i>Pharmacokinetics</i> of {{PAGENAME}} in the drug label.
|PK=*Papaverine is effective by all routes of administration. A considerable fraction of the drug localizes in fat deposits and in the liver, with the remainder being distributed throughout the body. *It is metabolized in the liver. About 90% of the drug is bound to [[plasma protein]]. Although estimates of its biologic [[half-life]] vary widely, reasonably constant plasma levels can be maintained with oral administration at 6 hour intervals. The drug is excreted in the urine in an inactive form.
 


<!--Nonclinical Toxicology-->
<!--Nonclinical Toxicology-->
|nonClinToxic=There is limited information regarding <i>Nonclinical Toxicology</i> of {{PAGENAME}} in the drug label.
|nonClinToxic=There is limited information regarding <i>Nonclinical Toxicology</i> of Papaverine in the drug label.


<!--Clinical Studies-->
<!--Clinical Studies-->
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of Papaverine in the drug label.


<!--How Supplied-->
<!--How Supplied-->
|howSupplied=*  
|howSupplied=* Papaverine Hydrochloride Injection, USP, 30 mg/mL
 
:*0517-4002-25              2 mL Vial                                packaged in boxes of 25
:*0517-4010-01              10 mL Multiple Dose Vial*    packaged individually
 
:*The 10 mL Multiple Dose Vial contains [[chlorobutanol]] 0.5% as a preservative.


<!--Patient Counseling Information-->
<!--Patient Counseling Information-->
|fdaPatientInfo=There is limited information regarding <i>Patient Counseling Information</i> of {{PAGENAME}} in the drug label.
|storage=*Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) (See USP Controlled Room Temperature).
*PROTECT FROM LIGHT. RETAIN IN CARTON UNTIL TIME OF USE.
|fdaPatientInfo=There is limited information regarding <i>Patient Counseling Information</i> of Papaverine in the drug label.


<!--Precautions with Alcohol-->
<!--Precautions with Alcohol-->
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|alcohol=* Alcohol-Papaverine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.


<!--Brand Names-->
<!--Brand Names-->
|brandNames=* ®<ref>{{Cite web | title =  | url =  }}</ref>
|brandNames=*Papacon
 
*Para-Time S.R.
*Pavacot
<!--Look-Alike Drug Names-->
<!--Look-Alike Drug Names-->
|lookAlike=* A® — B®<ref name="www.ismp.org">{{Cite web  | last =  | first =  | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>
|lookAlike=* A® — B®<ref name="www.ismp.org">{{Cite web  | last =  | first =  | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>
Line 267: Line 172:
}}
}}
{{LabelImage
{{LabelImage
|fileName={{PAGENAME}}11.png
|fileName=Papaverine 02.png
}}
}}
{{LabelImage
{{LabelImage
|fileName={{PAGENAME}}11.png
|fileName=Papaverine 03.png
}}
}}
<!--Pill Image-->
<!--Pill Image-->

Latest revision as of 17:05, 19 January 2015

Papaverine
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]; Associate Editor(s)-in-Chief: Aparna Vuppala, M.B.B.S. [2]

Disclaimer

WikiDoc MAKES NO GUARANTEE OF VALIDITY. WikiDoc is not a professional health care provider, nor is it a suitable replacement for a licensed healthcare provider. WikiDoc is intended to be an educational tool, not a tool for any form of healthcare delivery. The educational content on WikiDoc drug pages is based upon the FDA package insert, National Library of Medicine content and practice guidelines / consensus statements. WikiDoc does not promote the administration of any medication or device that is not consistent with its labeling. Please read our full disclaimer here.

Overview

Papaverine is a phosphodiesterase inhibitor that is FDA approved for the treatment of vascular spasm associated with acute myocardial infarction (coronary occlusion), angina pectoris, peripheral vascular disease, peripheral and pulmonary embolism. Common adverse reactions include general discomfort, nausea, abdominal discomfort, anorexia, skin rash, malaise, vertigo and headache..

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

  • Papaverine Hydrochloride may be administered intravenously or intramuscularly. The intravenous route is recommended when an immediate effect is desired, but the drug must be injected slowly over the course of 1 or 2 minutes to avoid uncomfortable or alarming side effects.
  • Parenteral administration of papaverine hydrochloride in doses of 1 to 4 mL is repeated every 3 hours as indicated. In the treatment of cardiac extrasystoles, 2 doses may be given 10 minutes apart.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

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


Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Safety and effectiveness in children have not been established.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

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

Non–Guideline-Supported Use

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

Contraindications

Complete atrioventricular heart block
Impotence

Warnings

Precautions

  • Papaverine Hydrochloride Injection, USP, should not be added to Lactated Ringer’s Injection, because precipitation would result.
  • Papaverine Hydrochloride should be used with caution in patients with glaucoma. The medication should be discontinued if hepatic hypersensitivity with gastrointestinal symptoms, jaundice, or eosinophilia becomes evident or if liver function test values become altered.
  • Drug dependence resulting from the abuse of many of the selective depressants, including papaverine hydrochloride, has been reported.

Adverse Reactions

Clinical Trials Experience

  • Hepatitis, probably related to an immune mechanism, has been reported infrequently. Rarely, this has progressed to cirrhosis.

Postmarketing Experience

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

Drug Interactions

There is limited information regarding Papaverine Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C

  • No teratogenic effects were observed in rats when papaverine hydrochloride was administered subcutaneously as a single agent. It is not known whether papaverine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. *Papaverine Hydrochloride should be given to a pregnant woman only if clearly needed.


Pregnancy Category (AUS): 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

  • It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when papaverine hydrochloride is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in children have not been established.

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

  • Intravenously or Intramuscularly

Monitoring

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

IV Compatibility

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

Overdosage

Signs and Symptoms
Management
  • To obtain up-to-date information about the treatment of overdose, a good resource is your certified Regional Poison Control Center. In managing overdosage, consider the possibility of multiple drug overdoses, interaction among drugs, and unusual drug kinetics in your patient.
  • No specific antidote is known.
  • Treatment should be symptomatic and supportive.
  • Protect the patient’s airway and support ventilation and perfusion. Meticulously monitor vital signs, blood gases, blood chemistry values, and other variables.

Pharmacology

This image is provided by the National Library of Medicine.

Mechanism of Action

  • The most characteristic effect of papaverine is relaxation of the tonus of all smooth muscle, especially when it has been spasmodically contracted. Papaverine Hydrochloride apparently acts directly on the muscle itself. This relaxation is noted in the vascular system and bronchial musculature and in the gastrointestinal, biliary and urinary tracts.
  • The main actions of papaverine are exerted on cardiac and smooth muscle. Papaverine relaxes various smooth muscles, especially those of larger arteries; this relaxation may be prominent if spasm exists. The antispasmodic effect is a direct one and unrelated to muscle innervation, and the muscle still responds to drugs and other stimuli causing contraction. Papaverine has minimal actions on the central nervous system, although very large doses tend to produce some sedation and sleepiness in some patients. In certain circumstances, mild respiratory stimulation can be observed, but this is therapeutically inconsequential. Papaverine stimulates respiration by acting on carotid and aortic body chemoreceptors.
  • Papaverine relaxes the smooth musculature of the larger blood vessels, including the coronary, cerebral, peripheral, and pulmonary arteries. This action is particularly evident when such vessels are in spasm, induced reflexly or by drugs, and it provides the basis for the clinical use of papaverine in peripheral or pulmonary arterial embolism.
  • Experimentally in dogs, the alkaloid has been shown to cause fairly marked and long-lasting coronary vasodilatation and an increase in coronary blood flow. However, it also appears to have a direct inotropic effect and, when increased mechanical activity coincides with decreased systemic pressure, increases in coronary blood flow may not be sufficient to prevent brief periods of hypoxic myocardial depression.

Structure

  • Papaverine Hydrochloride, USP, is the hydrochloride of an alkaloid obtained from opium or prepared synthetically. It belongs to the benzylisoquinoline group of alkaloids. It does not contain a phenanthrene group as do morphine and codeine.
  • Papaverine Hydrochloride, USP, is 6,7-dimethoxy-1- veratrylisoquinoline hydrochloride and contains, on the dried basis, not less than 98.5% of C20H21NO4•HCI. The molecular weight is 375.85. The structural formula is as shown.
This image is provided by the National Library of Medicine.
  • Papaverine Hydrochloride occurs as white crystals or white crystalline powder. One gram dissolves in about 30 mL of water and in 120 mL of alcohol. It is soluble in chloroform and practically insoluble in ether.
  • Papaverine Hydrochloride Injection, USP, is a clear, colorless to pale-yellow solution.
  • Papaverine Hydrochloride, for parenteral administration, is a smooth-muscle relaxant that is available in vials containing 30 mg/mL. Each vial also contains edetate disodium 0.005%. The 10 mL vials also contain chlorobutanol 0.5% as a preservative. pH may be adjusted with sodium citrate and/or citric acid.

Pharmacodynamics

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

Pharmacokinetics

  • Papaverine is effective by all routes of administration. A considerable fraction of the drug localizes in fat deposits and in the liver, with the remainder being distributed throughout the body. *It is metabolized in the liver. About 90% of the drug is bound to plasma protein. Although estimates of its biologic half-life vary widely, reasonably constant plasma levels can be maintained with oral administration at 6 hour intervals. The drug is excreted in the urine in an inactive form.

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

  • Papaverine Hydrochloride Injection, USP, 30 mg/mL
  • 0517-4002-25 2 mL Vial packaged in boxes of 25
  • 0517-4010-01 10 mL Multiple Dose Vial* packaged individually
  • The 10 mL Multiple Dose Vial contains chlorobutanol 0.5% as a preservative.

Storage

  • Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) (See USP Controlled Room Temperature).
  • PROTECT FROM LIGHT. RETAIN IN CARTON UNTIL TIME OF USE.

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

  • Papacon
  • Para-Time S.R.
  • Pavacot

Look-Alike Drug Names

Drug Shortage Status

Price

References

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

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

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