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methylergonovine (Methergine)

 

Classes: Ergot Derivatives

Dosing and uses of Methergine (methylergonovine)

 

Adult dosage forms and strengths

injectable solution

  • 0.2mg/mL

tablet

  • 0.2mg

 

Postpartum Hemorrhage

0.2 mg IM/IV q2-4hr PRN; not to exceed 5 doses, THEN 0.2-0.4 mg PO q6-8hr PRN for 2-7 days

Administer IV only in emergency because of potential for Hypertension & CVA

Administer over >1 minute and monitor Bp

 

Refractory Cluster Headache (Off-label)

0.2 mg PO q6-8hr, not to exceed 6 months

 

Pediatric dosage forms and strengths

Not applicable

 

Methergine (methylergonovine) adverse (side) effects

Frequency not defined

Nausea/vomiting

Dizziness

Headache

Tinnitus

Diaphoresis

Palpitation

Transient chest pain

Dyspnea

Thrombophlebitis

Hematuria

Water intoxication

Hallucinations

Leg cramps

Nasal congestion

Diarrhea

Foul taste

Allergic phenomena including shock

Hypertension

 

Postmarketing reports

Nervous system: Cerebrovascular accident, paraesthesia

Cardiovascular: Ventricular fibrillation, ventricular tachycardia, angina pectoris, atrioventricular block

 

Warnings

Contraindications

(All not necessarily unanimous): Hypertension, heart disease, toxemia, pregnancy, hypersensitivity, mitral valve stenosis, prolonged use

Cases of threatened spontaneous abortion

Avoid during breastfeeding

 

Cautions

Second or third stage of labor prior to placenta delivery: complications such as captivation of placenta may occur; avoid accidental injection to newborn babies

Increased risk of myocardial ischemia and infarction with coronary artery disease or risk factors for coronary artery disease

Sepsis, hepatic impairment, renal impairment, peripheral vascular disease

Prolonged use may cause pleuropulmonary, cardiac or retroperitoneal fibrosis

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Excreted in milk; adverse effect on nursing infant; may inhibit lactation; not recommended

Wait at least 12 hours after last dose to breastfeed

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Methergine (methylergonovine)

Mechanism of action

Produces vasoconstriction to increase strength, duration, & frequency of uterine contraction which in turn impedes uterine blood flow

 

Pharmacokinetics

Bioavailability: 60% (PO); 78% (IM)

Peak Plasma Time: 30 min

Peak Plasma Concentration: 3 ng/mL

Onset: uterine contractions are usually initiated within 5-15 min following oral administration, within 2-5 min after IM injection, & immediately following IV injection

Duration: 3 hr (PO); 3hr (IM); 45 min (IV)

Vd: 39-73L

Metabolism: Liver

Excretion: Urine and feces

Half-Life

  • Initial phase: 1-5 min
  • Terminal phase: 0.5-2 hr

 

Administration

IV Administration

Give IV only in emergency because of potential for HTN & CVA

Give over >1 min & monitor BP & uterine contractions