Midazolam metabolism is carried out rapidly by hepatic and small intestine cytochrome P450 (CYP3A4) enzymes to active and inactive metabolites. The principal metabolite of midazolam is 1-hydroxymidazolam, which has approximately half the activity of the parent compound. This active midazolam metabolism is rapidly conjugated to 1-hydroxymidazolam glucuronide and is subsequently cleared by the kidneys. This […]
The most commonly used barbiturate is pentobarbital. Induced coma with use of barbiturates like thiopentone sodium or pentothal is called barbiturate coma or pentobarbital coma . High-dose barbiturates have been used for more than 60 years in critically ill neurologic patients. The most common application has been to lower elevated intracranial pressure (ICP) in patients
All barbiturates metabolism is in the liver. In Barbiturates metabolism , the haemodilution in cardiopulmonary bypass (CPB) causes reduction in total drug concentration and protein binding fraction at the onset of CPB. This decrease in protein binding is counteracted by the dilution of unbound drug, resulting in a stable unbound concentration throughout CPB. The inactive metabolites
Flumazenil is the first specific benzodiazepine antagonist, used as a specific antidote in known or suspected benzodiazepine overdose treatment . In addition, flumazenil could be employed to reverse sedation produced by benzodiazepines during general anesthesia and prolonged sedation in intensive care units. Flumazenil is a specific and competitive antagonist at the central benzodiazepine receptor, reversing
Ketamine produces effective sedation, hence also known as Ketamine sedation . In pediatric patients for short surgical procedures or for putting intravenous catheters before IV induction ketamine has shown effective for producing sedation. It is highly effective with a wide margin of safety, and uniquely preserves protective airway reflexes and also does not require intravenous
Benzodiazepines effects appear to produce all their pharmacologic effects by facilitating the actions of gamma-amino butyric acid (GABA). The area where it causes it effect is the principal inhibitory neurotransmitter in the CNS by enhancing their affinity towards GABA receptors leading to increased chloride conductance and hyperpolarization of the postsynaptic cell membrane, and thereby rendering
At sub anesthetic doses, propofol anticonvulsant has been effectively used to suppress seizures during refractory status epilepticus, a mechanism, in part, attributed to the inhibition of neuronal sodium channels. It is effective in most patients, and the side effects are infrequent, of minor severity, and fully reversible. However, high doses of propofol may be necessary
Interventional techniques of musculoskeletal chronic pain management include use of nerve blocks, root blocks, rhizotomies, cordotomy, etc. Musculoskeletal chronic pain management is required during the following : 1. Low back pain – Lumbosacral, spinal/vertebral syndromes – Radiculopathy – Prolapsed intervertebral disc – Lumbar canal stenosis 2. Neuropathies: Trigeminal neuralgias (Tic doloroux) 3. Phantom limb pain,
The Etomidate brand name in common use is Amidate. Amidate is a carboxylated imidazole compound. The imidazole nucleus renders etomidate, like midazolam, water soluble at an acidic pH and lipid soluble at physiologic pH. It is a non-barbiturate hypnotic without analgesic properties that has less cardiovascular and respiratory depressant actions than sodium thiopental. This lipophilic
For the phenobarbital metabolism the binding of thiopentone in human serum is about 85% and remarkably constant over the concentration range between 4 and 80 micrograms/mL. The higher percentage of protein binding occurs at lower plasma concentrations of thiopental In phenobarbital metabolism . The percentage binding increases with increasing pH from approximate 75% at pH
