Mephentermine

Mephentermine
Clinical data
Routes of
administration
IM/IV
ATC code C01CA11 (WHO)
Pharmacokinetic data
Metabolism Rapidly demethylated in the body followed by hydroxylation.
Excretion Via urine (as unchanged and metabolites); more rapid in acidic urine.
Identifiers
Synonyms methyl(2-methyl-1-phenylpropan-2-yl)amine
CAS Number 100-92-5 YesY
PubChem (CID) 3677
IUPHAR/BPS 7222
DrugBank DB01365 YesY
ChemSpider 3549 YesY
UNII TEZ91L71V4 YesY
KEGG D08180 YesY
ChEMBL CHEMBL1201234 N
ECHA InfoCard 100.002.638
Chemical and physical data
Formula C11H17N
Molar mass 163.259 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Mephentermine is a cardiac stimulant. It was formerly used in Wyamine nasal decongestant inhalers and before that as a stimulant in psychiatry.

It has been used as a treatment for low blood pressure.[1]

ATC Classification: C01CA11 - mephentermine ; Belongs to the class of adrenergic and dopaminergic cardiac stimulants excluding glycosides. Used in the treatment of heart failure.

Mechanism of Action

Mephentermine appears to act by indirect stimulation of β-adrenergic receptors causing the release of norepinephrine from its storage sites. It has a positive inotropic effect on the myocardium. AV conduction and refractory period of AV node is shortened with an increase in ventricular conduction velocity. It dilates arteries and arterioles in the skeletal muscle and mesenteric vascular beds, leading to an increase in venous return.

Onset: 5–15 minutes (IM), immediate (IV).

Duration: 4 hr (IM), 30 minutes (IV).

Indication & Dosage

Maintenance of blood pressure in hypotensive states Adult: 30–45 mg as a single dose, repeated as necessary or followed by IV infusion of 0.1% mephentermine in 5% dextrose, rate and duration of administration will depend on patient's response.

Hypotension secondary to spinal anaesthesia in obstetric patients Adult: 15 mg as a single dose, repeat if needed.Maximum dose 30 mg.

Caution

Contraindications

Low blood pressure caused by phenothiazines. Hypertension. Pheochromocytoma.

Special Precautions

Patient on MAOIs. For shock due to loss of blood or fluid, give fluid replacement therapy primarily, CVS disease, hypertension, hyperthyroidism, chronic illnesses, lactation, pregnancy.

Adverse Drug Reactions

Drowsiness, incoherence, hallucinations, convulsions, slow heart rate (Reflex Bradycardia). Fear, anxiety, restlessness, tremor, insomnia, confusion, irritability, and psychosis. Nausea, vomiting, reduced appetite, urinary retention, dyspnea, weakness.

Potentially Fatal: AV block, CNS stimulation. Cerebral hemorrhage and pulmonary edema, ventricular arrhythmias.

Drug Interactions

Antagonizes effect of agents that lower blood pressure. Severe hypertension with MAOIs and possibly tricyclic antidepressants. Additive vasoconstricting effects with ergot alkaloids, oxytocin.

Potentially Fatal: Risk of abnormal heart rhythm in people undergoing anesthesia with cyclopropane and halothane.

References

  1. WHITTINGTON RM (May 1963). "Mephentemine Sulphate as a Hypertensive Agent in General Practice". J Coll Gen Pract. 6 (2): 336–7. PMC 1878111Freely accessible. PMID 14000433.


This article is issued from Wikipedia - version of the 4/27/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.