brands

Class

• Neuroscience-based Nomenclature: GABA positive allosteric modulator (GABA-PAM)
• Benzodiazepine (hypnotic)

Medistat commonly prescribed for

(Bold for FDA approved)

How Medistat works

• Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex

• Enhances the inhibitory effects of GABA

• Boosts chloride conductance through GABA-regulated channels

• Inhibitory actions in sleep centers may provide sedative hypnotic effects

How long until Medistat works

• Intravenous injection: onset 3–5 minutes

• Intramuscular injection: onset 15 minutes, peak 30–60 minutes

Notable Side Effects

• Oversedation, impaired recall, agitation, involuntary movements, headache

• Nausea, vomiting

• Hiccups, fluctuation in vital signs, irritation/ pain at site of injection

• Hypotension

Life Threatening Side Effects

• Respiratory depression, apnea, respiratory arrest

• Cardiac arrest

weight gain

unusual

sedation

common

What to do about Medistat side effects

• Wait

• Switch to another agent

• Administer flumazenil if side effects are severe or life-threatening

usual dosage range

• Intravenous (adults): 1–2.5 mg

• Liquid (age 16 and under): 0.25–1.0 mg/kg

Dosage Forms

• Syrup 2 mg/mL

• Nasal 5 mg/spray

• Intravenous 1 mg/mL, 5 mg/mL

• Intramuscular solution 50 mg/10 mL (5 mg/mL)

long term use

• Not generally intended for long-term use

habit forming

• Some patients may develop dependence and/or tolerance; risk may be greater with higher doses

• History of drug addiction may increase risk of dependence

Renal Impairment

• May have longer elimination half-life, prolonging time to recovery

Hepatic Impairment

• Longer elimination half-life; clearance is reduced

Cardiac Impairment

• Longer elimination half-life; clearance is reduced

Elderly

• Longer elimination half-life; clearance is reduced

• Intravenous: 1–3.5 mg; maximum 1.5 mg within 2 minutes

Children and Adolescents

• In most pediatric populations, pharmacokinetic properties are similar to those in adults

• Seriously ill neonates have reduced clearance and longer elimination half-life

• Hypotension has occurred in neonates given midazolam and fentanyl

• Intravenous dose: dependent on age, weight, route, procedure

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• Midazolam crosses the placenta

• Neonatal flaccidity has been reported in infants whose mother took a benzodiazepine during pregnancy

Breast Feeding

• Some drug is found in mother’s breast milk

• Effects on infant have been observed and include feeding difficulties, sedation, and weight loss

• Midazolam can be used to relieve postoperative pain after cesarean section