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Class: Vasodilating Agents, Miscellaneous
VA Class: CV900
CAS Number: 61-25-6
Brands: Para-Time SR

Medically reviewed by Last updated on Sep 21, 2020.


Vasodilating agent;180 181 a benzylisoquinoline alkaloid180 181 a prepared synthetically or obtained from opium.a

Uses for Papaverine

Cardiac and Vascular Uses

Relief of cerebral and peripheral ischemia associated with arterial spasm and myocardial ischemia complicated by arrhythmias.180 181 a

Has been used IV and intra-arterially in treatment of acute vascular occlusion in conjunction with anticoagulants.a

Treatment of angina pectoris;181 results not impressive at usual dosages.a Not recommended as a substitute for nitroglycerin in anginal attacks.a

Has been used in the treatment of other cardiovascular or vascular conditions including vascular encephalopathy associated with hypertensive disease, certain cerebral angiospastic states, and chronic peripheral vascular diseases (i.e., Raynaud’s syndrome, Buerger’s disease); however, use in these conditions has been superseded by more effective agents.a

Erectile Dysfunction

Self-treatment of erectile dysfunction (ED, impotence).178

Has been used alone or in combination with phentolamine and/or alprostadil in patients with neurogenic103 105 106 108 110 112 113 115 116 118 119 120 128 129 132 and/or limited vasculogenic impotence 103 105 106 108 110 112 113 115 116 120 121 128 129 132 or those with psychogenic impotence,105 106 108 120 128 129 132 but efficacy in patients with a vasculogenic component of their impotence may be variable depending on the extent and type of vascular dysfunction.103 108 110 115 120 128 129

The goal of therapy is to provide an erection of adequate rigidity and duration to be sexually functional while avoiding prolonged erection or priapism.142 143 144 145 146 147

Some experts (American Urological Association [AUA]) recommend that selective phosphodiesterase (PDE) type 5 inhibitor therapy (sildenafil, tadalafil, vardenafil) be offered as first-line erectile dysfunction treatment unless contraindicated.178

Intracavernosal therapy with papaverine and/or other drugs generally reserved for patients who do not respond to psychotherapy/behavioral therapy, vacuum constriction devices, and/or selective PDE type 5 inhibitors and in whom attempts at identifying and modifying any drug-related (e.g., certain antihypertensive agents) or other potential reversible medical cause of erectile dysfunction have proved inadequate.110 130

Some clinicians currently prefer alprostadil, alone or combined with other agents, when intracavernosal treatment of impotence is indicated because of possible improved efficacy and decreased adverse effects (e.g., priapism, fibrotic changes) compared with papaverine therapy.130 149 150 151 152 153 154

Choice of therapy for erectile dysfunction should be individualized taking into account differences in response, tolerability and safety, administration considerations, cost and patient reimbursement factors, experience and judgment of the clinician, and individual patient and partner preference, expectations, and satisfaction.170 171 172 173 174 175 176 177 178

Do not use for enhancing erections in men who are not impotent.154

Other Uses

Has been used in the treatment of GI spasms, dysmenorrhea, biliary or ureteral colic, bronchial asthma, cardiac arrhythmias, and other pathologic conditions;181 a however, insufficient evidence to establish therapeutic value.a

Papaverine Dosage and Administration


Administer orally, or by IM or slow IV injection.180 181 a

Has been used intra-arterially in treatment of acute vascular occlusion in conjunction with anticoagulants.a

Has been administered by intracavernous injection for the treatment of erectile dysfunction.103 105 106 107 108 110 112 113 114 115 116 118 119 120 121 122 123 124 125 126 127

IV Administration

Slow IV injection preferred when an immediate effect is desired.181 a

Rate of Administration

Inject slowly over a 1- to 2-minute period to minimize serious adverse effects (e.g., arrhythmias, fatal apnea).181 a (See Cardiovascular and Respiratory Effects under Cautions.)


Available as papaverine hydrochloride; dosage expressed in terms of salt.180 181

Pediatric Patients

Cardiac and Vascular Use†
IV or IM

6 mg/kg daily (as 4 divided doses).a


Cardiac and Vascular Use

Usually, 150 mg (extended-release capsules) every 8–12 hours.180 a

Alternatively, 300 mg (extended-release capsules) every 12 hours.a

75–300 mg (conventional tablets [no longer commercially available in US] 3–5 times daily, also has been used.a

IV or IM

Usually, 30 mg; may repeat 30–120 mg every 3 hours as necessary.181 a

Cardiac extrasystoles: May administer 2 doses 10 minutes apart.181 a

Erectile Dysfunction†
Intracavernosal Self-injection†

2.5–37.5 mg.178 Usually, titrated up to 30 mg in combination with phentolamine mesylate 0.5–1 mg (range: 0.08–1.25 mg).178

Tolerance with long-term use may require dosage increase.105 114 129

Prescribing Limits


Cardiovascular Use

960 mg daily.

Special Populations

No special population dosage recommendations at this time.180 181

Cautions for Papaverine


  • Complete atrioventricular heart block.181 a

  • Administer with extreme caution when cardiac conduction is depressed, because of increased risk of transient ectopic rhythms of ventricular origin (premature beats or paroxysmal tachycardia).181 a



Cardiovascular and Respiratory Effects

Administer IV slowly with caution; rapid injection may result in arrhythmias and fatal apnea.a

Large parenteral doses can depress atrioventricular and intraventricular conduction; may result in serious arrhythmias.180

Vasoactive Therapy

While some manufacturers have stated that papaverine hydrochloride injection is not indicated for the treatment of impotence via intracorporeal injection,133 134 135 181 the drug has been employed effectively via intracavernosal injection.103 105 106 107 108 110 112 113 114 115 116 118 119 120 121 126 128 130 132 137 142

Do not use vasoactive therapy for impotence in patients who might have conditions predisposing to priapism (e.g., sickle cell anemia or trait, multiple myeloma, leukemia), in those with anatomic deformation of the penis (e.g., angulation, cavernosal fibrosis, Peyronie’s disease), or in men in whom sexual activity is inadvisable or contraindicated.110 143 152 154 164 165 167 Discontinue vasoactive therapy in patients who develop penile angulation, cavernosal fibrosis, or Peyronie’s disease during therapy.143 167

Intracavernosal therapy (administered by self-injection) may be problematic in those receiving anticoagulants, who cannot tolerate transient hypotension, and those with poor manual dexterity, poor vision, or severe psychiatric disease.130

Priapism Associated with Intracavernosal Injection

Consider possibility of persistent priapism (a medical emergency) associated with intracavernosal injection; may require immediate medical and/or surgical intervention.103 105 106 107 108 110 113 115 116 120 122 125 127 129 130 131 132 137 178 181 a (See Advice to Patients.)

The risk of priapism can be reduced by careful patient instruction and dosage titration.132 137 142

Management of priapism includes aspiration of cavernosal blood105 110 113 115 116 120 127 129 and/or intracavernous injection of an α-adrenergic agonist (e.g., metaraminol, phenylephrine) or dopamine.103 105 106 107 108 109 110 111 113 115 120 127 129 137 179 Rarely, more radical therapy for priapism (e.g., cavernospongiosus or Winter’s shunt) may be necessary,104 105 106 110 129 179 such as in patients with persistent priapism (e.g., longer than 24 hours).104 110

Sensitivity Reactions

Hepatic Hypersensitivity

Hepatic hypersensitivity with GI symptoms, jaundice, eosinophilia, and altered hepatic function tests results reported.180 181 a

If such hypersensitivity occurs, discontinue the drug.180 181 a

General Precautions

Adequate Patient Monitoring

Administer papaverine injection only under the supervision of qualified clinician.181 a


Use with caution in patients with glaucoma.180 181 a

Abuse and Dependence

Potential abuse and dependence to papaverine reported.181 a

Specific Populations


Category C.181


Not known whether papaverine distributes into human milk.181 a Use with caution in nursing women.181 a

Pediatric Use

Safety and efficacy of papaverine in pediatric patients not established.181 a

However, children have received papaverine hydrochloride dosages of 6 mg/kg daily, divided into 4 IM or IV doses.a

Common Adverse Effects

Following oral administration: Nausea,a abdominal distress,180 a anorexia,180 a constipation,180 a malaise,180 a drowsiness,a vertigo,180 a sweating,180 a headache,180 a diarrhea,180 a rash,180 a flushing of the face,180 a increased heart rate,180 a increased depth of respirations,180 a slight increase in BP,180 a sedation.181 a

Following IV administration: General discomfort,181 nausea,181 abdominal discomfort,181 anorexia,181 constipation,181 diarrhea,181 skin rash,181 malaise,181 headache,181 flushing,181 sweating,181 sedation,181 hepatitis,181 hypotension,181 hypertension,181 thrombosis at IV injection site.a

Following intracavernosal administration: Priapism,103 105 106 107 108 110 113 115 116 120 122 125 127 129 130 131 132 137 178 transient pain,105 108 110 129 referred glans pain,108 110 129 burning,103 paresthesia.105 110 129

Interactions for Papaverine

Specific Drugs




CNS depressants

Possible increased papaverine effects a


Papaverine may block dopamine receptors and interfere with the therapeutic effects of levodopa a

Avoid concomitant use; do not use in patients with Parkinson's diseasea


Possible synergisma

Papaverine Pharmacokinetics



Readily absorbed from GI tract.a


Fairly rapid.a

Following intracavernosal injection, erectile response usually occurs within 10 minutes.105 106 108 112 113 114 116 118 119 129 132


Oral administration of extended-release capsules may provide continuous drug release over a 12-hour period.a

Following intracavernosal injection, erectile response may persist for 1 to several hours.105 106 108 112 113 114 116 118 119 129 132

Plasma Concentrations

Constant plasma concentrations can be maintained with oral administration at 6-hour intervals.181 a



Distributed throughout the body, with highest concentrations in fat deposits and liver.181

Not known if papaverine distributes into human milk.181 a

Plasma Protein Binding

90%.181 a



Rapidly metabolized in the liver.181 a

Elimination Route

Excreted in urine,181 a principally as inactive metabolites.181





15–30°C.180 a Protect from moisture.180



15–30°C.181 a Protect from light; keep in the original carton until time of use.181


For information on systemic interactions resulting from concomitant use, see Interactions.


Solution Incompatibility

Do not add papaverine hydrochloride injection to lactated Ringer’s injection because a precipitate would result.181 a


  • Main therapeutic action is a direct spasmolytic effect on smooth muscles.180 181 a

  • Spasmolytic effect most pronounced on blood vessels including the coronary, cerebral, pulmonary, and peripheral arteries; also relaxes smooth muscles of the bronchi, GI tract, ureters, and biliary system.180 181 a

  • Relaxes cardiac muscle by directly depressing the excitability of the myocardium, prolonging the refractory period, and depressing conduction.180 181 a

  • In the presence of vascular occlusion, may act by overcoming reflex vasoconstriction in collateral vessels.a

  • Direct vasodilating action on cerebral blood vessels may explain benefit reported in cerebral vascular encephalopathy.180

  • Minimal CNS actions;180 a although large doses may have a depressant effect.181 a

  • Weak calcium-channel activity with high doses.181 a

  • Little, if any, analgesic action.a

Advice to Patients

  • Advise patients receiving the drug via intracavernosal injection of potential for prolonged erections (priapism) and steps to take in the event that this serious adverse effect occurs.132 142 178 179

  • Importance of seeking immediate medical attention if an erection persists >4 hours or is extremely painful.132 142

  • Instruct patients receiving the drug via intracavernosal injection to visit their clinician regularly (e.g., at 3-month intervals) to assess therapeutic benefit, including the need for possible dosage adjustment, and of potential adverse effects associated with such therapy.143 147 159 167

  • Importance of informing clinicians if risk factors for cardiovascular disease are present prior to initiating any treatment.a

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.180 181

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.180 181

  • Importance of informing patients of other important precautionary information.180 181 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Papaverine Hydrochloride


Dosage Forms


Brand Names





Capsules, extended-release

150 mg*

Papaverine Hydrochloride Capsules ER


Para-Time SR




30 mg/mL*

Papaverine Hydrochloride Injection (with chlorobutanol 0.5% in multiple-dose vials or preservative-free in single-dose vials)

American Regent, Bedford

AHFS DI Essentials™. © Copyright 2021, Selected Revisions October 1, 2008. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.


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