Details About Overdose or Poisoning Generic Salt ::  Bromocriptine

Bromocriptine

    

Drug Pharmacology ::

I. Pharmacology. Bromocriptinemesylate is a semisynthetic derivative of the ergopeptide group ofergot alkaloids with dopaminergic agonist effects. It also has minoralpha-adrenergic antagonist properties. The dopaminergic effectsaccount for its inhibition of prolactin secretion and its beneficialeffects in the treatment of parkinsonism, neuroleptic malignantsyndrome (NMS; see Seizures), and cocaine craving as well as itsadverse effect profile and drug interactions. A key limitation is theinability to administer bromocriptine by the parenteral route coupledwith poor bioavailability (only about 6% of an oral dose is absorbed).In addition, the onset of therapeutic effects (eg, alleviation ofmuscle rigidity, hypertension, and hyperthermia) in the treatment ofNMS may take several hours to days.

Drug Indications ::

Indications

   

Treatment of NMS caused by neuroleptic drugs (eg, haloperidol and other antipsychotics) or levodopa withdrawal. Note: If the patient has significant hyperthermia (eg, rectal or core temperature 40°C[104°F]), bromocriptine should be considered secondary and adjunctivetherapy to immediate measures such as neuromuscular paralysis andaggressive external cooling.

Bromocriptinehas been used experimentally to alleviate craving for cocaine. However,a Cochrane database review (2003) concluded that current research doesnot support the use of dopamine agonists for treatment of cocainedependence. Caution: There is one case report of asevere adverse reaction (hypertension, seizures, and blindness) whenbromocriptine was used in a cocaine abuser during the postpartum period.

Note: Bromocriptine is notconsidered appropriate first-line therapy for acute drug-inducedextrapyramidal or parkinsonian symptoms (see Dystonia, dyskinesia, andrigidity).

Drug Contra-Indications ::

III. Contraindications./b>

   

Uncontrolled hypertension or toxemia of pregnancy.

Known hypersensitivity to the drug.

Arelative contraindication is a history of angina, myocardialinfarction, stroke, vasospastic disorders (eg, Raynaud’s disease), orbipolar affective disorder. In addition, there is no publishedexperience in children less than 7 years old. Children may achievehigher blood levels and require lower doses.

Drug Adverse Effects ::

IV. Adverse effects. Most adverse effects are dose-related and of minor clinical consequence; some are unpredictable.

   

The most common side effect is nausea. Epigastric pain, dyspepsia, and diarrhea also have been reported.

Hypotension(usually transient) and syncope may occur at the initiation oftreatment, and hypertension may occur later. Other cardiovasculareffects include dysrhythmias (with high doses), exacerbation of anginaand vasospastic disorders such as Raynaud’s disease, and intravascularthrombosis resulting in acute myocardial infarction (one case report).

Nervoussystem side effects vary considerably and include headache, drowsiness,fatigue, hallucinations, mania, psychosis, agitation, seizures, andcerebrovascular accident. Multiple interrelated risk factors includedose, concurrent drug therapy, and preexisting medical and psychiatricdisorders.

Rareeffects include pulmonary toxicity (infiltrates, pleural effusion, andthickening) and myopia with long-term, high-dose treatment (months).There has been one case of retroperitoneal fibrosis.

E. Use in pregnancy. FDAcategory B (see Table III–1). This drug has been used therapeuticallyduring the last trimester of pregnancy for treatment of a pituitarytumor. It has been shown to inhibit fetal prolactin secretion, and itmay precipitate premature laband inhibit lactation in the mother.

Drug Lab Interactions ::

Drug or laboratory interactions

   

Bromocriptine may accentuate hypotension in patients receiving antihypertensive drugs.

Theoretically,this drug may have additive effects with other ergot alkaloids, and itspotential to cause peripheral vasospasm may be exacerbated bypropranolol.

Bromocriptine may reduce ethanol tolerance.

Therehas been one case report of apparent serotonin syndrome (see Serotoninsyndrome) in a patient with Parkinson’s disease who received levodopaand carbidopa.

Drug Dose Management ::

Dosage and method of administration for NMS. Inadults, administer 2.5–10 mg orally or by gastric tube 3–4 times daily(average adult dose 5 mg every 8 hours). May increase to a maximum of20 mg every 6 hours. The pediatric dose is unknown (one case report of0.08 mg/kg every 8 hours in a 7-year-old; the tablets were mixed in a2.5-mg/10 mL slurry and given by feeding tube). Use small, frequentdosing to minimize nausea.

   

A therapeutic response usually is achieved with total daily doses of 5–30 mg.

Continuetreatment for 7–10 days after control of rigidity and fever, thenslowly taper the dose over 3 days (to prevent recurrence). Several daysof therapy may be required for complete reversal of NMS.

Drug Chemical Formulations ::

Formulations

   

Oral. Bromocriptine mesylate (Parlodel, others), 2.5-mg scored (SnapTabs) tablets and 5-mg capsules.

The suggested minimum stocking level to treat a 70-kg adult for the first 24 hours is 30 mg, or one 30-tablet (SnapTabs) package.

Disclaimer ::

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