Pharmacology: Metharbital, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
Mechanism Of Action: Metharbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.
Interactions:
DrugBank: Interactions for Metharbital
Interactions for Metharbital:
Interactions may occur with the following: adrenocorticoids (cortisone-like
medicine), anticoagulants (blood thinners), carbamazepine, corticotropin (barbiturates may decrease the effects of
these medicines), central nervous system (CNS) depressants (using these medicines with barbiturates may result in
increased CNS depressant effects), divalproex sodium, valproic acid (using these medicines with barbiturates may
change the amount of either medicine that you need to take), and oral contraceptives (birth control pills) containing
estrogens (barbiturates may decrease the effectiveness of these oral contraceptives, and you may need to change to a
different type of birth control).
Chemical IUPAC Name: 5,5-diethyl-1-methyl-hexahydropyrimidine-2,4,6-trione
Chemical Formula: C9H14N2O3
Half Life: Not Available
Drug Type: Approved Drug
# Accession No: APRD00757
CAS Registry Number: 50-11-3
Metharbital News (When available)
Mylan Laboratories and Forest Laboratories Announce Nebivolol ...Jan 12, 2006 PharmaLive.com (press release), ...and maintenance treatment of major depressive disorder and for generalized anxiety disorder in adults; Namenda(R) (memantine HCl), an N- methyl-D-aspartate ...
