- March 15, 2022
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Brand Name :
Loftran
Synonyms :
ketazolam
Class :
Benzodiazepine
Dosage Forms & Strengths
Capsule
15mg
30mg
45mg
Administer 15 to 60mg as a single dose or divided doses orally at bedtime
Administer 15 to 60mg as a single dose or divided doses orally at bedtime.
Safety and efficacy not established
Refer adult dosing
may increase the risk of CNS depression when combined with 1,2-Benzodiazepine
may increase the risk of CNS depression when combined with 1,2-Benzodiazepine
may increase the risk of CNS depression when combined with 1,2-Benzodiazepine
may increase the risk of CNS depression when combined with 1,2-Benzodiazepine
may increase the risk of CNS depression when combined with 1,2-Benzodiazepine
may increase the serum concentration when combined with each other
may increase the serum concentration when combined with each other
may increase the serum concentration when combined with each other
may increase the serum concentration when combined with each other
may decrease the serum concentration when combined with each other
may decrease the excretion rate when combined with each other
may decrease the excretion rate when combined with each other
may increase the risk of adverse effects when combined with each other
may increase the risk of adverse effects when combined with each other
may diminish the excretion rate of each other when combined
may diminish the metabolism of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
it increases the toxicity of antipsychotic agents
may have an increasingly adverse effect when combined with antipsychotic agents
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
may increase the effect of beta-blockers
may reduce the therapeutic effect of antiparkinson drugs
may reduce the therapeutic effect of antiparkinson drugs
may reduce the therapeutic effect of antiparkinson drugs
may reduce the therapeutic effect of antiparkinson drugs
may reduce the therapeutic effect of antiparkinson drugs
may have an increased hypotensive effect when combined with beta-blockers
may have an increased hypotensive effect when combined with beta-blockers
may have an increased hypotensive effect when combined with beta-blockers
may have an increased hypotensive effect when combined with beta-blockers
may have an increased hypotensive effect when combined with beta-blockers
may increase the risk of adverse effect of amphetamines
may increase the risk of adverse effect of amphetamines
may increase the risk of adverse effect of amphetamines
may increase the risk of adverse effect of amphetamines
may increase the risk of adverse effect of amphetamines
The potential for increased CNS depression risk or seriousness occurs when ketazolam is used together with pinazepam
The potential for increased CNS depression risk or seriousness occurs when ketazolam is used together with pipecuronium
The potential for CNS depression may enhanced when ketazolam is used together with fencamfamin
It may increase the neurotoxic effect of Antipsychotic Agents
antipsychotic agents may enhance the adverse/toxic effect of amphetamines
antipsychotic agents may enhance the adverse/toxic effect of amphetamines
antipsychotic agents may enhance the adverse/toxic effect of amphetamines
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
may increase the hypotensive effect of beta-blockers
may increase the hypotensive effect of beta-blockers
may increase the hypotensive effect of beta-blockers
may increase the hypotensive effect of beta-blockers
may increase the hypotensive effect of beta-blockers
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the effect of antipsychotic agents
may enhance the effect of antipsychotic agents
may enhance the effect of antipsychotic agents
may enhance the effect of antipsychotic agents
may enhance the effect of antipsychotic agents
eprosartan/hydrochlorothiazide
may increase the hypotensive effect of blood pressure-lowering agents
may increase the hypotensive effect of blood pressure-lowering agents
may decrease the therapeutic effect when combined with antipsychotic agents
may have an increased adverse effect when combined with antipsychotic agents
it increases the toxicity of antipsychotic agents
may increase the arrhythmogenic effect of Inhalational Anaesthetics
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may have an increasingly adverse effect when combined with amphetamines
may enhance the hypotensive effect of Blood Pressure Lowering Agents
may diminish the absorption when combined
metyrosine: they may increase the toxic effect of antipsychotic agents
may decrease the therapeutic effect of each other when combined
Acetylcholinesterase Inhibitors: they may increase the neurotoxic effect of antipsychotics
Acetylcholinesterase Inhibitors: they may increase the neurotoxic effect of antipsychotics
Could potentially amplify the neurotoxicity of antipsychotic agents
The potential for arrhythmogenic effects of mequitazine could be intensified by the presence of antipsychotic agents
Actions and Spectrum:
ketazolam, like other benzodiazepines, exerts its effects primarily by enhancing the inhibitory actions of a neurotransmitter called gamma-aminobutyric acid (GABA) in the central nervous system. GABA is the primary inhibitory neurotransmitter in the brain, and its activation leads to decreased neuronal excitability, helping to reduce anxiety, induce sedation, and promote muscle relaxation.
Benzodiazepines, including ketazolam, bind to specific sites on GABA-A receptors, which are ion channels in the brain that allow chloride ions to enter neurons. This influx of chloride ions hyperpolarizes the neuron’s membrane potential, making it less likely for the neuron to generate an action potential (an electrical signal that allows neurons to communicate). This overall inhibition of neural activity contributes to ketazolam’s anxiolytic, sedative, and muscle relaxant effects.
ketazolam is primarily used for its anxiolytic (anxiety-reducing) effects. It can help manage various anxiety disorders, including generalized and panic disorders. It may also be used to manage symptoms of alcohol withdrawal due to its soothing properties.
Frequency not defined
Confusion
Diminished reflexes
Somnolence
Coma
Black box warning:
None
Contraindications/caution:
Contraindications:
Caution:
Pregnancy consideration: Insufficient data available
Lactation: Excretion of the drug in human breast milk is unknown
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
<b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
Pharmacokinetics:
Absorption
ketazolam is available in oral formulations, typically in the form of tablets. It is well-absorbed from the gastrointestinal tract after oral administration. Absorption is influenced by factors such as the drug’s formulation, the presence of food, and individual variations in gastrointestinal physiology.
Distribution
Once absorbed into the bloodstream, ketazolam is distributed throughout the body, including the central nervous system (CNS), due to its lipophilic nature. It crosses the blood-brain barrier and enters the CNS, where it exerts its pharmacological effects by enhancing GABAergic neurotransmission.
Metabolism
ketazolam undergoes metabolism primarily in the liver. It is metabolized by various cytochrome P450 enzymes, particularly CYP3A4. The primary metabolites formed are hydroxylated derivatives of ketazolam. These metabolites are generally pharmacologically inactive. The metabolic process transforms ketazolam into more water-soluble compounds, facilitating their elimination from the body.
Elimination and Excretion
ketazolam and its metabolites are eliminated from the body primarily through the urinary system. They are excreted in the urine, with a portion of the drug and its metabolites being eliminated unchanged and the rest as metabolites. The elimination half-life of ketazolam is approximately 24 hours on average, but this can vary based on factors such as age, liver function, and other individual factors.
Administration:
Oral administration
The dosage of ketazolam and the frequency of administration can vary depending on the condition being treated, the individual’s response to the medication, and other factors. Generally, ketazolam is taken orally with water, and the tablets should not be crushed or chewed.
Patient information leaflet
Generic Name: ketazolam
Why do we use ketazolam?
ketazolam is a benzodiazepine derivative with several medical uses primarily related to its anxiolytic (anti-anxiety), sedative, muscle relaxant, and anticonvulsant properties.
