Papaverine (Lexi-Drugs Multinational)

Pronunciation

(pa PAV er een)

Brand Names: International

Atrophen (LI); Mesotina (LI); Paparin (IN); Papaverini (ID); Papaverinum Hydrochloricum (PL);

Papaverol (EC); Tropaverin (LI)

Anatomic Therapeutic Chemical (ATC) Classification

A03AD01
G04BE02

Pharmacologic Category
Dosing: Adult

Vasodilator

Note: Labeled uses have fallen out of favor; safer and more effective alternatives are available. The manufacturers

labeling recommends the following dosing:

Arterial spasm: IM, IV: 30-120 mg; may repeat dose every 3 hours; if cardiac extrasystole occurs during use, may administer 2 doses 10
minutes apart
* See Dosage and Administration in AHFS Essentials for additional information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

No dosage adjustment provided in the manufacturers labeling.

Dosing: Hepatic Impairment

Use: Labeled Indications

No dosage adjustment provided in the manufacturers labeling.

Various vascular spasms associated with smooth muscle spasms as in myocardial infarction, angina,

peripheral and pulmonary embolism, peripheral vascular disease; cerebral angiospastic states; visceral spasms (ureteral, biliary, and GI
colic). Note: Labeled uses have fallen out of favor; safer and more effective alternatives are available.
* See Uses in AHFS Essentials for additional information.

Use: Off-Label
Prevention of vasospasm during harvesting mammary arteries for coronary artery bypass graft surgery

Administration: IV

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

Administration: Injectable Detail

Dietary Considerations
Storage/Stability

May be taken with food.

Store at 20C to 25C (68F to 77F); excursions permitted to 15C to 30C (59F to 86F). Protect from light.

Preparation for Administration

Compatibility

pH: Not <3; 3-4 (2% solution in water)

Solutions should be clear to pale yellow. Precipitates with lactated Ringer's.

Stable in D5LR, D51/4NS, D51/2NS, D5NS, D5W, D10W, 1/2NS, NS; incompatible with LR.

Compatibility in syringe: Compatible: Iohexol 64.7%, iopamidol 61%, iothalamate sodium 60%, phentolamine. Variable (consult detailed
reference): Ioxaglate meglumine 39.3%, ioxaglate sodium 19.6%.

Medication Safety Issues

Sound-alike/look-alike issues:
Papaverine may be confused with pamidronate
Geriatric Patients: High-Risk Medication:

Beers Criteria: Vasodilators (papaverine) are identified in the Beers Criteria as potentially inappropriate medications to be used
with caution in patients 65 years and older with a history of syncope due to its potential to exacerbate episodes of syncope
(Beers Criteria [AGS 2015]).

Contraindications

Patients with complete AV block

Warnings/Precautions
Concerns related to adverse effects:
Arrhythmias: May (in large doses or with rapid infusion) depress AV and intraventricular cardiac conduction leading to serious
arrhythmias (eg, premature beats, paroxysmal tachycardia).
Hepatitis: May cause hepatic hypersensitivity; discontinue use if GI symptoms, jaundice, eosinophilia, or abnormal LFTs occur.
Disease-related concerns:
Glaucoma: Use with caution in patients with glaucoma.
Other warnings/precautions:
Appropriate use: Not indicated for treatment of impotence by intracorporeal injection; persistent priapism may occur.
* See Cautions in AHFS Essentials for additional information.

Geriatric Considerations

The use of vasodilators for cognitive dysfunction is not recommended or proven by appropriate

scientific study.

Pregnancy Risk Factor: US

Pregnancy Considerations

Teratogenic effects have not been observed in animal reproduction studies.

Breast-Feeding Considerations

It is not known if papaverine is excreted in breast milk. The manufacturer recommends that

caution be exercised when administering papaverine to nursing women.

Adverse Reactions

Frequency not defined.

Cardiovascular: Arrhythmias (with rapid IV use), flushing, mild hypertension, tachycardia

Central nervous system: Headache, malaise, sedation, vertigo
Dermatologic: Rash
Gastrointestinal: Abdominal distress, anorexia, constipation, diarrhea, nausea
Hepatic: Cirrhosis, hepatic hypersensitivity, hepatitis (rare)
Respiratory: Apnea (with rapid IV use)
Miscellaneous: Diaphoresis
* See Cautions in AHFS Essentials for additional information.

Allergy and Idiosyncratic Reactions

Benzylisoquinoline Allergy

Metabolism/Transport Effects
Drug Interactions

None known.
Open Interactions

Levodopa: Papaverine may enhance the hypotensive effect of Levodopa. Papaverine may diminish the therapeutic effect of Levodopa.
Risk C: Monitor therapy

Monitoring Parameters

Blood pressure, heart rate

Monitoring Parameters

Blood pressure, heart rate

Nursing: Physical Assessment/Monitoring

Use caution in presence of glaucoma. IV, IM: Blood pressure and heart rate

should be monitored. IV: Should be administered slowly (over 1-2 minutes) to avoid apnea or arrhythmias. Monitor for arrhythmias,
tachycardia, hypertension, and GI disturbance.

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Injection, as hydrochloride:

Generic: 30 mg/mL (2 mL, 10 mL)

Generic Available (US)

Yes

Pricing: US
Solution (Papaverine HCl Injection)
30 mg/mL (2 mL): $3.36
Disclaimer: The pricing data provide a representative AWP and/or AAWP price from a single manufacturer of the brand and/or generic
product, respectively. The pricing data should be used for benchmarking purposes only, and as such should not be used to set or
adjudicate any prices for reimbursement or purchasing functions. Pricing data is updated monthly.

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
Bioavailability: Oral: ~54%
Half-life elimination: 30 to 120 minutes
Excretion: Primarily urine (as metabolites)

Local Anesthetic/Vasoconstrictor Precautions

Effects on Dental Treatment
Effects on Bleeding

No information available to require special precautions

No significant effects or complications reported

No information available to require special precautions

Related Information
Beers Criteria Potentially Inappropriate Medications for Geriatrics
Drug-Induced Prolongation of the QT Interval and Torsades de Pointes

Index Terms

Papaverine Hydrochloride; Pavabid

References
American Geriatrics Society 2015 Beers Criteria Update Expert Panel. American Geriatrics Society 2015 updated Beers Criteria for
potentially inappropriate medication use in older adults. J Am Geriatr Soc. 2015;63(11):2227-2246. doi:10.1111/jgs.13702[PubMed
26446832]
Girard DS, Sutton JP, Williams TH, et al, Papaverine Delivery to the Internal Mammary Artery Pedicle Effectively Treats Spasm, Ann

Thorac Surg, 2004, 78(4):1295-8.[PubMed 15464488]

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. [PubMed 8504648]
Ilan Y and Gemer O, Papaverine-Induced Coma, Eur J Clin Pharmacol, 1988, 33(6):651. [PubMed 3366170]
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.
Yavuz S, Celkan A, Goncu T, et al, Effect of Papaverine Applications on Blood Flow of the Internal Mammary Artery, Ann Thorac
Cardiovasc Surg, 2001, 7(2):84-8.[PubMed 11398777]

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