papaverine

REMS

Although designated by the FDA as ineffective for these indications, has been used in the following:
- Management of cerebral and peripheral ischemia, usually associated with arterial spasm,
- Treatment of myocardial ischemia complicated by arrhythmias,
- Improvement of collateral circulation in acute vascular occlusion,
- Management of ureteral, biliary, or GI colic.

Unlabeled Use: Intracavernosal

Adjunct treatment (with alpha-adrenergic blockers) in the management of male erectile dysfunction from organic causes.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity or complete AV block.

Use Cautiously in:

Glaucoma;
Depressed cardiac conduction;
Priapism;
Sickle cell disease;
Impaired liver function;
Severe coagulation defects;
OB: Pregnancy, lactation, or children (safety not established).

Adv. Reactions/Side Effects ⬆ ⬇

CV: arrhythmias (IV only), hypotension, slight hypertension

Derm: flushing, sweating

EENT: dry throat, visual changes

GI: abdominal distress, anorexia, constipation, diarrhea, dry mouth, hepatitis, nausea

GU: priapism (intracavernosal only)

Local: thrombosis at injection site

Neuro: depression, dizziness, drowsiness, headache, sedation, vertigo

Resp: APNEA (IV ONLY)

Interactions ⬆ ⬇

Drug-drug:

May prevent response tolevodopa in patients with Parkinson’s disease.
Alpha-adrenergic agonists (metaraminol, epinephrine, or phenylephrine) or cigarette smoking (nicotine) may reverse the vasodilating effects of papaverine.

Availability ⬆ ⬇

(Generic available)

Tablets: 100 mg
Extended-release capsules: 150 mg
Injection: 30 mg/mL in 2- and 10-mL ampules; 32.5 mg/mL

Route/Dosage ⬆ ⬇

PO (Adults ): 150 mg q 12 hr, up to 150 mg q 8 hr or 300 mg q 12 hr.
Intracavernosal(Adults ): 30 mg with 0.5–1 mg of phentolamine or 30 mg alone initial dose, may increase to 60 mg/dose, not to be repeated more than 3 times/wk or more than 2 consecutive days).

US Brand Names ⬆ ⬇

Papacon, Para-Time S.R., Pavacot

Action ⬆ ⬇

Dilation of arteries by a direct spasmolytic action on vascular smooth muscle.

Therapeutic effects:

Vasodilation.

Classifications ⬆ ⬇

Therapeutic Classification: erectile dysfunction agents

Pharmacologic Classification: vasodilators

Pharmacokinetics ⬆ ⬇

Absorption: Variably (50%) absorbed after oral administration; absorption from timed-release formulations may be less. Slowly absorbed after intracavernosal administration.

Distribution: Unknown.

Protein Binding: 90%.

Metabolism/Excretion: Mainly metabolized by the liver.

Half-Life: 0.5–2 hr (highly variable; may be as long as 24 hr).

Time/Action Profile ⬆ ⬇

(PO, IM, IV = vasodilating effects, intracavernosal = penile erection)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	unknown	4–8 hr
PO-ER	unknown	unknown	8–12 hr
IV	unknown	unknown	3 hr
Intracavernosal	10 min	unknown	4 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed. Take missed dose as soon as remembered, but not if almost time for next dose. Do not double doses. Instruct patient not to discontinue medication without conferring with health care professional.
Encourage patient not to smoke; concurrent administration of nicotine will cause vasoconstriction.
May cause dizziness or drowsiness. Advise patient to avoid driving or other activities requiring alertness until response to medication is known.
Caution patient to make position changes slowly to minimize orthostatic hypotension.
Instruct patient to notify health care professional if dizziness, drowsiness, jaundice, or vision changes occur.
Advise patients with a history of glaucoma to have regular eye examinations.

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Indications ⬇