Drug information of Quazepam

Quazepam


It is used to treat sleep problems.

Mechanism of effect

Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization. Benzodiazepine receptors and effects appear to be linked to the GABA-A receptors. Benzodiazepines do not bind to GABA-B receptors.

Pharmacodynamic

Metabolism
Hepatic via CYP3A4, CYP2C9, and CYP2C19 (Fukasawa, 2004; Kato, 2003); forms metabolites (active) 2-oxoquazepam and N-desalkyl-2-oxoquazepam
Absorption
Rapid
Excretion
Urine (31%, only trace amounts as unchanged drug); feces (23%)
Time to Peak
~2 hours
Half life
Serum: Quazepam, 2-oxoquazepam: 39 hours; N-desalkyl-2-oxoquazepam: 73 hours

Drug indications

Insomnia: For the treatment of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning

Dosage

Usual Adult Dose for Insomnia
Initial dose: 7.5 mg orally once a day at bedtime
Maintenance dose: 7.5 to 15 mg orally once a day at bedtime

Drug contraindications

Hypersensitivity to quazepam, other benzodiazepines, or any component of the formulation; established or suspected sleep apnea; pulmonary insufficiency

Side effects

>10%
 Central nervous system: Daytime sedation
<10%
Central nervous system: Headache (5%), dizziness (2%), fatigue (2%)
Gastrointestinal: Xerostomia (2%), dyspepsia (1%)
Frequency not defined.
Cardiovascular: Palpitations
Central nervous system: Abnormality in thinking, agitation, amnesia, anxiety, apathy, ataxia, confusion, depression, drug dependence, euphoria, malaise, nervousness, nightmares, paranoia, speech disturbance
Dermatologic: Pruritus, skin rash
Endocrine & metabolic: Decreased libido
Gastrointestinal: Abdominal pain, anorexia, constipation, diarrhea, dysgeusia, nausea
Genitourinary: Impotence, urinary incontinence
Neuromuscular & skeletal: Hyperkinesia, hypokinesia, tremor, weakness
Ophthalmic: Cataract, visual disturbance
<1%, postmarketing, and/or case reports: Anaphylaxis, angioedema, sleep disorder (complex sleep-related behavior, eg, cooking while sleeping, eating food while sleeping, making phone calls while sleeping, sleep driving)

Alcohol (Ethyl), Alizapride, Azelastine (Nasal), Blonanserin, Brexanolone, Brimonidine (Topical), Bromopride, Bromperidol, Buprenorphine, Cannabidiol, Cannabis, CloZAPine,
Chlormethiazole, Chlorphenesin Carbamate, CNS Depressants, Dimethindene (Topical),
Doxylamine, Dronabinol, Droperidol, Esketamine, Flunitrazepam, Fosphenytoin,
HydrOXYzine, Kava Kava, Lemborexant, Lisuride, Lofexidine, Magnesium Sulfate,
Melatonin, Methadone, Methotrimeprazine, Metoclopramide, MetyroSINE, Minocycline (Systemic), Nabilone, OLANZapine, Opioid Agonists, Orphenadrine, Oxomemazine,
OxyCODONE, Paraldehyde, Perampanel, Phenytoin, Piribedil, Pramipexole, ROPINIRole,
Rotigotine, Rufinamide, Selective Serotonin Reuptake Inhibitors, Sodium Oxybate,
Suvorexant, Teduglutide, Tetrahydrocannabinol, Tetrahydrocannabinol and Cannabidiol,
Thalidomide, Theophylline Derivatives, Trimeprazine, Yohimbine, Zolpidem

Alerts

This medicine is a benzodiazepine. The use of a benzodiazepine drug along with opioid drugs has led to very bad side effects. Side effects that have happened include slowed or trouble breathing and death. Opioid drugs include drugs like codeine, oxycodone, and morphine. Opioid drugs are used to treat pain and some are used to treat cough. Talk with the doctor

If you are taking quazepam with an opioid drug, get medical help right away if you feel very sleepy or dizzy; if you have slow, shallow, or trouble breathing; or if you pass out. Caregivers or others need to get medical help right away if the patient does not respond, does not answer or react like normal, or will not wake up

May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness 

Postmarketing studies have indicated that the use of hypnotic/sedative agents for sleep has been associated with hypersensitivity reactions including anaphylaxis as well as angioedema. Patients that have developed angioedema should not be rechallenged with quazepam

Use caution in patients with depression, particularly if suicidal risk may be present


Points of recommendation

What do I need to tell my doctor BEFORE I take Quazepam
If you have any of these health problems: Breathing problems or sleep apnea
If you are taking any other drugs that can make you sleepy. There are many drugs that can do this. Ask your doctor or pharmacist if you are not sure

avoid driving and doing other tasks or actions that call for you to be alert after you take quazepam. You may still feel sleepy the day after you take quazepam. Avoid these tasks or actions until you feel fully awake

This medicine may be habit-forming with long-term use

When sleep drugs are used nightly for more than a few weeks, they may not work as well to help sleep problems. This is known as tolerance. Only use sleep drugs for a short time. If sleep problems last, call the doctor

Do not take quazepam for longer than you were told by your doctor

If you have been taking quazepam for more than 10 days, talk with your doctor before stopping. You may want to slowly stop quazepam

Avoid alcohol while taking quazepam. Do not take quazepam if you drank alcohol that evening or before bed

Talk with your doctor before you use other drugs and natural products that slow your actions

Some people have done certain tasks or actions while they were not fully awake like driving, making and eating food, and having sex. Most of the time, people do not remember doing these things. Tell your doctor if this happens to you

This medicine may make you feel sleepy and less alert. This may lead to falling. The chance of falling is higher in older people. If you have questions, talk with the doctor

If you are 65 or older, use quazepam with care. You could have more side effects

Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using quazepam while you are pregnant

Tell your doctor if you are breast-feeding or plan to breast-feed. This medicine passes into breast milk and may harm your baby

Take quazepam right before you get into bed

Do not take with or right after a meal

Do not take quazepam unless you can get a full night's sleep (at least 7 to 8 hours) before you need to be active again

Pregnancy level

D

D

Breast feeding warning

Avoid if breastfeeding

Drug forms

Doral

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