midterm benzodiazepines

Benzodiazepines

Drugs that work by enhancing a very important neurotransmitter called gamma-aminobutyric acid (GABA) at the GABA A receptor

Benzodiazepines

Drugs that result in sedative, hypnotic, anxiolytic, anticonvulsant, and muscle relaxant properties

GABA

Is the chief inhibitor neurotransmitter in the mammalian CNS

GABA

Neurotransmitter whose role is in reducing neuronal excitability and regulation of muscle tone

GABA-A receptors

GABA sends its inhibitory message by binding at special sites called __________

Chloride

Once GABA is bound to the GABA-A receptor, the neurons open a channel which allows __________ ions to pass inside of the neuron

Diazepam (Valium), Midazolam

__________ and __________ are benzodiazepines used for sedation during surgery and to treat seizures (DM)

Diazepam

__________ is also used to treat anxiety, alcohol withdrawal symptoms, and for relief of muscle spasms in some neurological diseases

Diazepam

Brand names for __________ include valium, diastat acudial, diastat, and diazepam intensol

Sedation, Drowsiness

Side effects of diazepam and midazolam that are similar include __________ and __________ (SD)

Diazepam

Unique side effects of __________ include fatigue, diarrhea, rash, euphoria, loss of balance, excitability, muscle spasm, lack of sleep, rage, confusion, speech problems, and double vision

Midazolam

Unique side effects of __________ include difficulty breathing, nausea, vomiting, and pain at the injection site

Diazepam, Midazolam

Withdrawal symptoms such as insomnia, headaches, nausea, vomiting, lightheadedness, sweating, anxiety, fatigue, and seizures may occur if you suddenly stop taking __________ or _________ (DM)

Midazolam

Contains a benzodiazepine ring fused with an imidazole ring (an imidazobenzodiazepine) (Diazepam or midazolam)

Midazolam

Has F atom on one phenyl ring (Diazepam or midazolam)

Both

Has Cl atom on the benzene ring (Diazepam or midazolam)

Midazolam

Contains an imidazole ring (5-membered ring with nitrogen atoms) which makes it water-soluble at acidic pH and lipid-soluble at physiological pH (Diazepam or midazolam)

Midazolam

Used as sedative and pre-anesthetic medication (Diazepam or midazolam)

Midazolam

Used for induction of anesthesia, conscious sedation, and seizure control (Diazepam or midazolam)

Midazolam

Short-acting duration (Diazepam or midazolam)

Midazolam

8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo (Diazepam or midazolam)

Diazepam

C16H13ClN2O (Diazepam or midazolam)

Diazepam

A classical benzodiazepine with a seven-membered diazepine ring fused to a benzene ring and attached to a phenyl ring (Diazepam or midazolam)

Diazepine

Contains a carbonyl group (C=O) on the diazepine ring (Diazepam or midazolam)

Diazepam

Has a methyl group (CH3) attached to a nitrogen atom (Diazepam or midazolam)

Diazepam

Treats anxiety, muscle spasms, seizures, and alcohol withdrawal (Diazepam or midazolam)

Diazepam

Used as a premedication before surgery (Diazepam or midazolam)

Diazepam

Long-acting duration (Diazepam or midazolam)

Diazepam

Is a benzodiazepine used to treat anxiety, alcohol withdrawal symptoms, seizures, for relief of muscle spasms in some neurological diseases, and for sedation during surgey

Midazolam

Is a benzodiazepine used for sedation

Benzodiazepines

Other __________ include lorazepam (Ativan), diazepam (Valium), alprazolam (Xanax), clonazepam (Klonopin), flurazepam (Dalmane), and others

Diazepam

Causes drowsiness, fatigue, diarrhea, rash, euphoria, and ataxia (Diazepam or midazolam)

Diazepam

Other important side effects include paradoxical reactions with excitability, muscle spasm, lack of sleep, rage, confusion, speech problems, and double vision (Diazepam or midazolam)

Diazepam

Possible serious side effects include respiratory depression, neutropenia, and depression (Diazepam or midazolam)

Midazolam

Causes sedation, difficulty breathing, nausea, vomiting, and pain at the injection site (Diazepam or midazolam)

Diazepam

May be taken with or without food (Diazepam or midazolam)

Diazepam

Is disposed of by the liver and excreted mainly by the kidney (Diazepam or midazolam)

2-10 mg given 2-4x daily

Usual oral diazepam dose for anxiety or seizures

0.2-0.5 mg/kg

Usual rectal dose for diazepam

Midazolam

Is given by intramuscular or intravenous injection (Diazepam or midazolam)

0.5-1 mg given over 2 mins (not to exceed 2.5 mg per dose)

Dose of midazolam for sedation during surgery

2-3

Doses of midazolam for sedation during surgery may be repeated after __________ to __________ minutes

5

Total midazolam doses greater than __________ mg usually are not needed

200-350 mcg/kg IV over 20-30 seconds

Dose of midazolam for starting anesthesia

Diazepam

Alcohol or medications that cause sedation may add to the sedative effects of __________

Prolong

Cimetidine, ketoconazole, itraconazole, omeprazole, and omeprazole may __________ the effects of diazepam (CYP450 inhibitors)

Decrease

Carbamazepine, rifampin, and St. John’s wort __________ levels of diazepam by increasing liver enzymes (CYP450 inducers)

Midazolam

__________ and all benzodiazepines interact with other medications that slow the brain’s processes

Increase

Boceprevir, itraconazole, nelfinavir, and telaprevir __________ blood level of midazolam by reducing its breakdown in the liver (CYP450 inhibitors)

Pregnancy

Benzodiazepines, including diazepam, can cause fetal abnormalities and should not be used during __________

Diazepam

__________ is excreted in breast milk and can affect nursing infants; therefore, diazepam should not be used by women who are nursing

Midazolam

__________ and other benzodiazepines have been associated with fetal damage

Midazolam

____________ is best avoided at all if possible in the first trimester and probably throughout pregnancy

Breast milk

Midazolam is secreted in __________