Papaverine

Pronunciation

(pa PAV er een)

U.S. Brand Names

Para-Time S.R.®

Synonyms

Papaverine Hydrochloride; Pavabid [DSC]

Generic Available

Yes

Use

Oral: Relief of peripheral and cerebral ischemia associated with arterial spasm and myocardial ischemia complicated by arrhythmias

Use - Unlabeled/Investigational

Investigational: Parenteral: Various vascular spasms associated with muscle spasms as in myocardial infarction, angina, peripheral and pulmonary embolism, peripheral vascular disease, angiospastic states, and visceral spasm (ureteral, biliary, and GI colic); testing for impotence

Pregnancy Risk Factor

Lactation

Excretion in breast milk unknown/not recommended

Contraindications

Hypersensitivity to papaverine or any component of the formulation

Warnings/Precautions

Use with caution in patients with glaucoma; administer I.V. cautiously since apnea and arrhythmias may result; may, in large doses, depress AV and intraventricular cardiac conduction leading to serious arrhythmias (eg, premature beats, paroxysmal tachycardia); chronic hepatitis noted with jaundice, eosinophilia, and abnormal LFTs

Adverse Reactions

Frequency not defined.

Cardiovascular: Arrhythmias (with rapid I.V. use), flushing of the face, mild hypertension, tachycardia

Central nervous system: Drowsiness, headache, lethargy, sedation, vertigo

Gastrointestinal: Abdominal distress, anorexia, constipation, diarrhea, nausea

Hepatic: Chronic hepatitis, hepatic hypersensitivity

Respiratory: Apnea (with rapid I.V. use)

Overdosage/Toxicology

Symptoms of overdose include nausea, vomiting, weakness, gastric distress, ataxia, hepatic dysfunction, drowsiness, nystagmus, hyperventilation, hypotension, and hypokalemia. Treatment is supportive.

Drug Interactions

Decreased effect: Papaverine decreases the effects of levodopa

Increased toxicity: Additive effects with CNS depressants

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase CNS depression).

Stability

Protect from heat or freezing; refrigerate injection at 2°C to 8°C (35°F to 46°F); solutions should be clear to pale yellow; precipitates with lactated Ringer's

Compatibility

Stable in dextran 6% in dextrose, dextran 6% in NS, D5LR, D5¹ /4NS, D5¹ /2NS, D5NS, D5W, D10W, ¹ /2NS, NS; not stable in LR

Compatibility in syringe: Compatible: Iohexol 64.7%, iopamidol 61%, iothalamate sodium 60%, metrizamide 48.25%, phentolamine. Incompatible: Diatrizoate meglumine 52%, diatrizoate sodium 8%. Variable (consult detailed reference): Diatrizoate meglumine 66%, diatrizoate sodium 10%, diatrizoate sodium 60%, ioxaglate meglumine 39.3%, ioxaglate sodium 19.6%

Compatibility when admixed: Compatible: Theophylline. Incompatible: Aminophylline with trimecaine

Mechanism of Action

Smooth muscle spasmolytic producing a generalized smooth muscle relaxation including: vasodilatation, gastrointestinal sphincter relaxation, bronchiolar muscle relaxation, and potentially a depressed myocardium (with large doses); muscle relaxation may occur due to inhibition or cyclic nucleotide phosphodiesterase, increasing cyclic AMP; muscle relaxation is unrelated to nerve innervation; papaverine increases cerebral blood flow in normal subjects; oxygen uptake is unaltered

Pharmacodynamics/Kinetics

Onset of action: Oral: Rapid

Protein binding: 90%

Metabolism: Rapidly hepatic

Half-life elimination: 0.5-1.5 hours

Excretion: Primarily urine (as metabolites)

Dosage

I.M., I.V.:

Children: 6 mg/kg/day in 4 divided doses

Adults: 30-65 mg (rarely up to 120 mg); may repeat every 3 hours

Oral, sustained release: Adults: 150-300 mg every 12 hours; in difficult cases: 150 mg every 8 hours

Administration

Rapid I.V. administration may result in arrhythmias and fatal apnea; administer no faster than over 1-2 minutes.

Dietary Considerations

May be taken with food.

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take as directed; do not alter dose or discontinue without consulting prescriber. Swallow extended release capsules whole; do not chew, crush, or dissolve. May cause dizziness, confusion, or blurred vision (avoid driving or engaging in tasks that require alertness until response to drug is known); or constipation (increased exercise, fluids, fruit, or fiber may help). Report rapid heartbeat or palpitations and CNS changes (eg, depression, persistent sedation or lethargy, or acute headache). Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.

Anesthesia and Critical Care Concerns/Other Considerations

The use of vasodilators for cognitive dysfunction is not recommended.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause drowsiness or dizziness

Mental Health: Effects on Psychiatric Treatment

May decrease the effects of levodopa

Dosage Forms

Capsule, sustained release, as hydrochloride (Para-Time SR®): 150 mg

Injection, solution, as hydrochloride: 30 mg/mL (2 mL, 10 mL)

References

Erwin WG, "Senile Dementia of the Alzheimer Type," Clin Pharm , 1984, 3(5):497-504.

Heulitt MJ, Farrington EA, O'Shea TM, et al, "Double-Blind, Randomized, Controlled Trial of Papaverine-Containing Infusions to Prevent Failure of Arterial Catheters in Pediatric Patients," Crit Care Med , 1993, 21(6):825-9.

Higbee MD, "Noncholinergic Approaches to Treating Senile Dementia of the Alzheimer's Type," Consult Pharm , 1992, 7(6):635-41.

Ilan Y and Gemer O, "Papaverine-Induced Coma," Eur J Clin Pharmacol , 1988, 33(6):651.

Jahr JS, Kang B, Paxtor CG, et al, "Hemodynamic Responses to Papaverine: Do Nitric Oxide, Cyclic GMP, or Calcium Mediate the Vasodilitation?" Am J Therapeut , 1995, 2(4):258-64.

Sillanpää M and Koponen M, "Papaverine in the Prophylaxis of Migraine and Other Vascular Headache in Children," Acta Paediatr Scand , 1978, 67(2):209-12.

Vaziri ND, Stokes J, and Treadwell TR, "Lactic Acidosis, A Complication of Papaverine Overdose," Clin Toxicol , 1981, 18(4):417-23.

Waters C, "Cognitive Enhancing Agents: Current Status in the Treatment of Alzheimer's Disease," Can J Neurol Sci , 1988, 15(3):249-56.

Yesavage JA, Tinklenberg JR, Hollister LE, et al, "Vasodilators in Senile Dementias: A Review of the Literature," Arch Gen Psychiatry , 1979, 36(2):220-3.

International Brand Names

Clorhidrat de Papaverina® (RO); Cloridrato de Papaverina® (BR); DBL Papaverine® (TH); Mesotina® (AR); Papaverina Clorhidrato® (CL); Papaverina Clorhidrat® (RO); Papaverina Clorhidrica® (RO); Papaverina Cloridrato® (IT); Papaverina Fada® (AR); Papaverina Hé Teofarma® (IT); Papaverina® (RO); Papaverine HCl® (IL); Papaverine Hydrochloride® (AU, IL, NZ, RU, SG); Papavérine Renaudin® (FR); Papavérine Serb® (FR); Papaverine® (TR); Papaverini HCL® (ID); Papaverin Oba® (DK); Papaverin Recip® (SE); Papaverin SAD® (DK); Papaverinum Hydrochloricum® (HU, PL); Verantrop® (VE)

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