|
|
|
Pronunciation |
|
(pa
PAV er
een) |
|
|
U.S. Brand
Names |
|
Genabid®; Pavabid®;
Pavatine® |
|
|
Generic
Available |
|
Yes |
|
|
Synonyms |
|
Papaverine Hydrochloride |
|
|
Pharmacological Index |
|
Vasodilator |
|
|
Use |
|
Oral: Relief of peripheral and cerebral ischemia associated with arterial
spasm and myocardial ischemia complicated by arrhythmias |
|
|
Pregnancy Risk
Factor |
|
C |
|
|
Contraindications |
|
Hypersensitivity to papaverine or its components |
|
|
Warnings/Precautions |
|
Use with caution in patients with glaucoma; administer I.V. cautiously since
apnea and arrhythmias may result; may, in large doses, depress A-V and
intraventricular cardiac conduction leading to serious arrhythmias (eg,
premature beats, paroxysmal tachycardia); chronic hepatitis noted with jaundice,
eosinophilia, and abnormal LFTs |
|
|
Adverse
Reactions |
|
<1%: Flushing of the face, tachycardias, mild hypertension, vertigo,
drowsiness, sedation, lethargy, headache, nausea, constipation, abdominal
distress, anorexia, diarrhea, hepatic hypersensitivity, chronic
hepatitis |
|
|
Overdosage/Toxicology |
|
Symptoms of acute overdose include nausea, vomiting weakness, gastric
distress, ataxia, drowsiness, nystagmus, diplopia, incoordination, lethargy, and
coma with cyanosis, and respiratory depression
After gastric decontamination, treatment is supportive with conventional
therapy (ie, fluids, positioning and vasopressors for hypotension)
|
|
|
Drug
Interactions |
|
CYP2D6 enzyme substrate
Increased toxicity: Additive effects with CNS depressants
|
|
|
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 |
|
|
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 in the liver
Half-life: 0.5-1.5 hours
Elimination: Primarily as metabolites in urine |
|
|
Usual Dosage |
|
Adults: Oral, sustained release: 150-300 mg every 12 hours; in difficult
cases: 150 mg every 8 hours |
|
|
Dietary
Considerations |
|
May be administered with food |
|
|
Mental Health: Effects
on Mental Status |
|
May cause drowsiness or dizziness |
|
|
Mental Health:
Effects on Psychiatric
Treatment |
|
May decrease the effects of levodopa |
|
|
Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
|
No information available to require special precautions |
|
|
Dental Health:
Effects on Dental Treatment |
|
No effects or complications reported |
|
|
Patient
Information |
|
Oral: Take as directed; do not alter dosage without consulting prescriber. Do
not chew, crush, or dissolve extended release tablets. Avoid alcohol while
taking this medication. May cause dizziness, confusion, or blurred vision (avoid
driving or engaging in tasks that require alertness until response to drug is
known). Increased fiber in diet, exercise, and adequate hydration (2-3 L/day of
fluids unless instructed to restrict fluid intake) may help if you experience
constipation. Report rapid heartbeat or palpitations, CNS depression, persistent
sedation or lethargy, or acute headache. Pregnancy/breast-feeding
precautions: Inform prescriber if you are or intend to be pregnant.
Breast-feeding is not recommended. |
|
|
Nursing
Implications |
|
Rapid I.V. administration may result in arrhythmias and fatal apnea;
administer slow I.V. over 1-2 minutes |
|
|
Dosage Forms |
|
Capsule, sustained release, as hydrochloride: 150 mg |
|
|
References |
|
Erwin WG, "Senile Dementia of the Alzheimer Type," Clin Pharm, 1984,
3:497-504.
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.
Ilan Y and Gemer O, "Papaverine-Induced Coma," Eur J Clin Pharmacol,
1988, 33(6):651.
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, 15:249-56.
Yesavage JA, Tinklenberg JR, Hollister LE, et al,
"Vasodilators in Senile Dementias: A Review of the Literature," Arch Gen
Psychiatry, 1979, 36:220-3. |
|
Copyright © 1978-2000 Lexi-Comp Inc. All Rights Reserved
| |