Drugs for Nervous System

ALPRAZOLAM

Class:

BENZODIAZEPINE DERIVATIVE

ANXIOLYTIC, SEDATIVE, HYPNOTIC

Pharmacokinetics :

Absorption :Rapid

Distribution : 0.9-1.2 L/kg (Vd)

Metabolism : Hepatic

Excretion : Urine

Indications & Dose:

ANXIETY :-

Acute Short-term therapy -

PO Adult 0.5-4mg/day in divided doses,

max 4mg/day

Elderly Initially 0.125-0.25mg BID, increase by 0.125mg/day

ANXIETY WITH DEPRESSION :

Acute Short-term therapy -

PO Adult 2.5-3mg/day in divided doses

PANIC DISORDER -

Acute Short-term therapy :

PO Adult Initially 0.5mg TID, dose may be increase q3-4 days in increments equivalent to 1 mg/day, effective dosage is 5-6mg/day

PREOPERATIVE SEDATION -

Acute PO Adult 0.5mg HS & 0.5mg 1h before procedure.

Contraindication :

Hypersensitivity, glaucoma, concomitant use with ketoconazole/itraconazole

Precautions:

Respiratory disease, hepatic/renal impairment, elderly, muscle weakness, myasthenia gravis, history of drug/alcohol abuse, marked personality disorder, avoid prolonged use & abrupt withdrawal, acute porphyria

ADR:

Serious: Respiratory depression, hypotension, jaundice, blurred vision, Others: agitation, incontinence, insomnia, irritability, libido, phlebitis, urinary retention, Confusion, dizziness, ataxia, fatigue, vertigo, constipation

DDI:

Serious Dexamphetamine behavioural effects is reduced, Ketoconazole decreases drug clearance and prolonged its half-life, Theophylline/Carbamazepine decreases drug level, Ritonavir increased sedative effects, Hormonal Contraceptives increases drug effects, Macrolides/Fluvoxamine increases drug level, Alcohol level increases and leads to enhance the CNS depressant effects, CCBs prolongs sedative & amnesic effects, Fluoxetine reduces the drug clearance.

DEXMEDETOMIDINE

Class:-

ALPHA2-ADRENOCEPTOR

SEDATIVE

Pharmacokinetics :

Absorption :Well absorbed

Distribution : Vd: 118L

Metabolism Hepatic

Excretion : Urine (95%); feces (4%)

Indications & Dose:

ICU SEDATION IV Adult 1mcg/kg over 10 min; MD: 0.2-1.4mcg/kg/hr, titrate less frequently than q30min to prevent hypotension

PROCEDURAL SEDATION :

Adult 1mcg/kg over 10 min; MD: 0.6mcg/kg/hr titrate to effect (usually 0.2-1mcg/kg/hr)

Contraindications :

Hypersensitivity

Precautions:

Renal/hepatic impairment, Risk of hypotension, bradycardia and sinus arrest, Cardiovascular disease, diabetes, and in patients receiving vasodilators

ADR:

Serious: Hypotension, Anemia, Bradycardia, Pulmonary edema,

Others: Fever

DIAZEPAM

Class:-

BENZODIAZEPINE

SEDATIVE, HYPNOTIC, ANXIOLYTIC

SKELETAL MUSCLE RELAXANT

Anti-Epileptics

Pharmacokinetics :

Absorption : Well absorbed

Distribution : 0.8-1 L/kg (Vd)

Metabolism : Hepatic

Excretion : Urine

Indications & Dose:

ANXIETY -

PO :

Adult 2-10mg 2-4 times/day

Child 0.12-0.8mg/kg/day in divided doses q6-8h

IV/IM :

Adult 2-10mg, repeat in 3-4h if needed

Child 0.04-0.3mg/kg/dose q2-4h, max 0.6mg/kg within an 8h period if needed

CONSCIOUS SEDATION FOR PROCEDURES

PO Child 0.2-0.3mg/kg max 10mg, 45-60 min before procedure

ETHANOL WITHDRAWAL Acute

PO Adult 10mg 3-4 times during first 24h,

then decrease to 5mg 3-4 times/day as needed

INSOMNIA ASSOCIATED WITH ANXIETY

Adult 5-15mg HS, max 30mg

MUSCLE SPASM Acute

IV/IM Adult Initially 5-10mg,

then 5-10mg in 3-4h,

larger dose may be required if condition is associated with tetanus

MUSCLE SPASM WITH TETANUS :

IV/IM Child Infants >30 days: 1-2mg/dose q3-4h as needed;

>5 yrs: 5-10mg/dose q3-4h as needed

NIGHT TERRORS :

PO Adult 1-5mg HS

SEDATION :

PO Child 0.12-0.8mg/kg/day in divided doses q6-8h

IV/IM:

Adult 0.03-0.1mg/kg q30min to 6h

Child 0.04-0.3mg/kg/dose q2-4h, max 0.6mg/kg within an 8h period if needed

SKELETAL MUSCLE RELAXANT :

Adjuvant therapy

PO Adult 2-10mg 3-4 times/day

Child 0.12-0.8mg/kg/day in divided doses q6-8h

SLEEPWALKING :

PO Adult 1-5mg HS

STATUS EPILEPTICUS :

Acute IV -

Adult 5-10mg q5-10mins given over <5mg/min, max 30mg

Child 0.1-0.3mg/kg given over <5mg/min, may repeat dose after 5-10mins, max 10mg/dose

Acute RECTAL -

Adult Gel: 10mg/day repeat once if needed

Child Gel: 0.5mg/kg, then 0.25mg/kg in 10mins if needed

Contraindications :

Hypersensitivity, myasthenia gravis, respiratory depression, hepatic impairment, sleep apnea, glaucoma

Precautions:

Respiratory disease, history of drug/alcohol abuse, marked personality disorder, hepatic/renal impairment, avoid prolonged use & abrupt withdrawal, acute porphyria

ADR:

Serious:

Respiratory depression, hypotension, jaundice

Others:

Drowsiness, fatigue, muscle weakness, ataxia, confusion, vertigo, constipation, blurred vision, dizziness, stimulation, agitation, insomnia, libido, urinary retention, phlebitis.

DDI:

Serious Etravirine increase drug levels, Rifampicin increases drug clearance, Fluvoxamine increases drug effect, Hormonal Contraceptives increases drug effects and may also increase the incidence of break-through bleeding, Alcohol increases drug level, Fentanyl increases risk of respiratory depression, Papaverine prolongs the erections, Isoniazid/Ciprofloxacin reduces drug clearance, Digoxin urinary clearance reduced Others Theophylline antagonizes drug effects, Phenytoin decreases drug level, Omeprazole/Modafinil/Valproic acid increases drug level.

Diet:

With/without food

Monitor:

Anxiety, BP, respiratory & CV status.

DOXYLAMINE

Class :

MONOETHANOLAMINE DERIVATIVE

SEDATIVE ANTI-HISTAMINE

Indications & Dose:

INSOMNIA

PO Adult 25mg given q4-6h, max 150mg/day

Contraindications :

Alcohol, CVD, known/suspected prolongation of QT interval, hypokalemia/electrolyte imbalances, neonates, topical application on broken/eczematous skin

Precautions:

Angle-closure glaucoma, urinary retention, prostatic hyperplasia, pyloroduodenal obstruction, epilepsy, hepatic impairment, young children, elderly.

ADR:

Serious: antimuscarinic effects, hypersensitivity reactions, convulsions, Others: myalgia, extrapyramidal effects, depression, hypotension, nausea, vomiting, diarrhea, epigastric pain, rash, CNS depression, headache, psychomotor impairment.

ESZOPICLONE

Class:

GABA ENHANCER

SEDATIVE, HYPNOTIC

Pharmacokinetics :

Absorption : Rapid

Metabolism :Hepatic

Excretion : Urine (75% as metabolites; <10% as parent drug)

Indications & Dose:

INSOMNIA : Short-term therapy

PO Adult 2mg HS, max 3mg

Elderly 1mg HS, max 2mg

Precautions:

Complex sleep-related behaviors, sensitivity reactions, abuse, comorbidities

ADR:

Serious: Allergic reactions, xerostomia, anaphylaxis, asthma, dysmenorrhea.

Others: nervousness, pruritus, libido, dyspepsia, diarrhea, dizziness, UTI, alopecia

DDI:

Serious Rifampicin decreases drug level, Itraconazole/Clarithromycin/Ketoconazole/Nelfinavir/Ritonavir increases drug level, AntiConvulsants results in additive effect

Diet: Avoid after heavy meal

Monitor:

Prior to therapy evaluate physical/psychiatric causes of insomnia.

ETIZOLAM

Class:

SHORT-ACTING BENZODIAZEPINE

SEDATIVE

Indications & Dose:

ANXIETY -

PO Adult 3mg/day in divided doses/single dose HS

INSOMNIA PO Adult 3mg/day in divided doses/single dose HS

FLURAZEPAM

Class:

LONG-ACTING BENZODIAZEPINE

SEDATIVE, HYPNOTIC

Pharmacokinetics :

Absorption : Rapid

Distribution : 3.4L/kg (Vd)

Metabolism : Hepatic

Excretion : Urine

Indications & Dose:

INSOMNIA - Short-term therapy

PO Adult 15-30mg HS <4wk

Child <15 yrs: Dose not established

>15 yrs: 15mg HS

Elderly 15mg HS

Contraindications :

hypersensitivity to flurazepam/other benzodiazepines, preexisting CNS depression, angle-closure glaucoma

Precautions:

Hepatic impairment, history of suicide attempt, drug dependence, elderly, children <15 yrs

ADR:

Serious:

Blurred vision, depression

Others: dizziness, daytime drowsiness, headache, confusion, paradoxical excitation, ataxia, nausea, vomiting, diarrhea, constipation, abdominal pain, sleep apnea, rash, abnormal taste, physical/ psychological drug dependence.

DDI:

Serious Clozapine causes severe hypotension, respiratory depression or loss of consciousness, HIV protease inhibitors increases drug bioavailability, Cimetidine increases drug level, Alcohol increases risk of drowsiness, impaired performance & driving skills

Diet:

Monitor:

Mental status, CBC, LFTs, kidney function tests

HYDROXYZINE

Class:

ANTI-HISTAMINE

ANTI-PRURITIC, ANXIOLYTIC

SEDATIVE & HYPNOTIC

Pharmacokinetics :

Absorption : Rapid

Distribution :

Metabolism :

Excretion :

Indications & Dose:

ANXIETY - Short-term therapy

PO -

Adult 50-100mg QID

Child <6 yr: 50mg/day in divided doses,

>6 yr: 50-100mg/day in divided doses

IM -

Adult Initially 50-100mg, then q4-6h as needed

PREOPERATIVE SEDATION

PO-

Adult 50-100mg Child 0.6mg/kg/dose

IM -

Adult 25-100mg

Child 0.5-1mg/kg/dose

PRURITUS

PO Adult 25mg TID/QID

Child 6 month-6 yr: Initially 5-15mg HS, increased to 50mg/day in 3-4 divided doses if required,

6-12 yr: Initially 15-25mg HS, increased to 50-100mg/day in 3-4divided doses if required, 12-18 yr: Initially 25mg HS, increased to 50-100mg/day in 3-4divided doses if required.

Contraindications :

Hypersensitivity, Sc/intra-arterial/IV administration

Precautions:

Narrow-angle glaucoma, prostatic hyperplasia and/or urinary stricture, asthma/COPD, bladder neck obstruction, elderly.

ADR:

Serious: hypersensitivity reaction

Others: pain/abscess at IM Inj site, drowsiness, agitation, dizziness, headache, asthenia, ataxia, nausea, constipation, dry mouth, urinary retention, wheezing, flushing, bitter taste.

DDI:

Serious Alcohol increases drowsiness effect of drug, Cimetidine moderately raises drug levels

Monitor: Adverse effects, LFTs

MELATONIN

Class:

PINEAL HORMONE

SUPPLEMENTARY DRUG

Indications & Dose:

INSOMNIA Short-term therapy

PO Adult > 55 yr: 2mg OD 1-2 hr before bedtime for 3wk

Contraindications :

hepatic impairment, autoimmune disease

Precautions: renal impairment

ADR:

Serious: hypertriglyceridemia, muscle cramps, nervousness, increased libido, blood disorders, Others: skin reaction, lacrimation, visual disturbances, irritability, sweating, flatulence, halitosis, hypersalivation, vomiting, aggression, agitation, fatigue, impaired memory, mood changes, hot flushes, priapism, pharyngitis, back pain, headache, asthenia, abdominal pain, constipation, dry mouth, weight gain, drowsiness, dizziness, sleep disorders, restlessness

DDI:

Serious Imipramine increases CNS effects, Fluvoxamine increases the drug level, Caffeine increases the drug levels, Oestrogens/Cimetidine slightly increases drug level

MIDAZOLAM

Class:

SHORT-ACTING BENZODIAZEPINE

SEDATIVE & HYPNOTIC

ADJUNCT FOR GENERAL ANESTHESIA INDUCTION

Pharmacokinetics :

Absorption : Rapid (PO)

Distribution : 1-3.1 L/kg (Vd)

Metabolism : Hepatic

Excretion : Urine & feces (2%-10%)

Indications & Dose:

CONSCIOUS SEDATION -

PO-

Child 0.25-0.5mg/kg single dose, max 20mg 30-60min before procedure

IV -

Adult Initially 0.5-2mg over 2min, repeat dose q2-3min if needed, reduce dose by 30% if narcotics/other CNS depressants used

Child Same as preoperative sedation

Elderly Initially 0.5mg slowly at least 2min

IM -

Child 0.1-0.15mg/kg 30-60min before surgery/procedure, max 10mg

INDUCTION OF ANESTHESIA

IV Adult Unpremedicated patients: 0.3-0.35mg/kg, premedicated patients: 0.15-0.35mg/kg MD 0.05-0.3mg/kg as needed

Child 7-18 yr: 150µg/kg slowly max 7.5mg given in steps of 50µg/kg max 2.5mg over 2-5min, additional doses of 50µg/kg max 2.5mg q2min if needed.

PREOPERATIVE SEDATION -

PO -

Child 0.25-0.5mg/kg single dose, max 20mg 30-60min before procedure

IV -

Adult 0.02-0.04mg/kg, repeat q5min max 0.1-0.2mg/kg

Child 6 months-5 yr: Initially 0.05-0.1mg/kg max total dose 6mg,

6-12 yr: Initially 0.025-0.05mg/kg max total dose 10mg,

12-16 yr: max 10mg

IM-

Adult 0.07-0.08mg/kg 30-60min before surgery/procedure

Child 0.1-0.15mg/kg 30-60 min before surgery/procedure, max 10mg

SEDATION IN INTESIVE CARE

Short-term therapy PO Adult 7.5-15mg HS

Contraindications :

Hypersensitivity, acute closed-angle glaucoma

Precautions:

Pulmonary disease, HF, renal/ severe hepatic impairment, obese child, elderly/debilitated patients, children/neonates

ADR:

Serious:

Hypotension, paradoxical reaction, seizure-like activity, decreased respiratory rate, phlebitis, bronchospasm

Others: acid taste, amnesia, bradycardia, tachycardia, drowsiness, over sedation, physical & psychological dependence, rash.

DDI:

Serious Verapamil/Diltiazem causes deep sleep & prolonged hypnosis, Carbamazepine decreases drug effect,Clarithromycin/Azithromycin/Erythromycin/Lopinavir/Nelfinavir/Ritonavir/Roxithromycin increases drug level, Azoles increases drug plasma level & increases sedation, Alcohol increases risk of drowsiness, impairs performance & driving skills Others Fentanyl causes respiratory depression, hypotension, Halothane potentiates anesthetic action of drug.

Diet:

Monitor: Respiratory & CV status, BP

NITRAZEPAM

Class :

BENZODIAZEPINE

SEDATIVE & HYPNOTIC, ANTI-EPILEPTIC

Pharmacokinetics :

Absorption :Rapid

Distribution : 2.4L/Kg (Vd)

Metabolism :Hepatic

Excretion :Urine (65%-70%), feces (14%-20%)

Indications & Dose:

INSOMNIA - Short-term therapy

PO Adult 5-10mg HS Elderly 2.5-5mg HS

MYOCLONIC SEIZURES -

PO Child <30 kg: 0.3-1mg/kg/day TID

Contraindications :

Porphyria, myasthenia gravis, narrow angle glaucoma, severe respiratory insufficiency, sleep apnea syndrome, severe hepatic impairment

Precautions: Respiratory disease, muscle weakness, history of drug/alcohol abuse, elderly/debilitated patients, renal impairment

ADR:

Serious:

Hypotension, blurred vision, psychoses

Others: aspiration, granulocytopenia, muscle weakness, constipation, diarrhea, nightmares, palpitation, delusion, change in libido, headache, irritability.

DDI:

Serious Rifampicin increases drug clearance, Hormonal Contraceptives increases drug effect, Primidone levels are reduced in children

Diet:

Monitor: Respiratory & cardiovascular status

PHENOBARBITAL

Class:

BARBITURATE SEDATIVE, HYPNOTIC,

ANTI-EPILEPTIC.

Pharmacokinetics :

Absorption : PO: 70-90%

Metabolic : Hepatic

Excretion : Urine (20-50% as unchanged drug)

Indications & Dose:

FEBRILE CONVULSIONS -

PO Child 8mg/kg/day

GENERALIZED TONIC-CLONIC SEIZURES -

PO Adult 60-180mg HS

Child 8mg/kg/day

HYPNOTIC -

PO - Adult 100-320mg HS

IV/IM - Adult 100-320mg HS

Child 3-5mg/kg HS

NEONATAL SEIZURES -

IV Child 5-10mg/kg q20-30mins up to plasma concentration of 40mg/L

PARTIAL SEIZURES -

PO Adult 60-180mg HS Child 8mg/kg/day

PREOPERATIVE SEDATION -

PO/IV Child 1-3mg/kg 1-1.5h before procedure

IM - Adult 100-200mg 1-1.5h before procedure Child 1-3 mg/kg 1-1.5h before procedure

SEDATION -

PO Adult 30-120mg/day in 2-3 divided doses.

Child 2mg/kg TID

IM - Adult 30-120mg/day in 2-3 divided doses

SEIZURES -

Acute Emergency therapy

IV - General 60mg/min

Acute Emergency therapy

IM - General 200mg q6h

STATUS EPILEPTICUS

IV - Adult Loading dose: 10-20mg/kg (max rate <60mg/min in patient’s >60 kg), repeat dose q20min if needed, max 30mg/kg

Child 15-20mg/kg (max rate <30 mg/min in children <60 kg), repeat dose after 15min as needed, max 40mg/kg

Contraindication :

Hypersensitivity to barbiturates, porphyria, severe hepatic impairment, absence seizures, airway obstruction, intra-arterial & SC administration, history of sedative/hypnotic addiction, nephritis

Precautions: Elderly/debilitated, children, renal impairment, respiratory depression, sudden withdrawal, rapid IV administration.

ADR:

Serious: Bradycardia, hypotension, exfoliative dermatitis, SJS, thrombophlebitis, laryngospasm, respiratory depression, oliguria, gangrene, CNS excitation/depression.

Others: Rash, syncope, dizziness, drowsiness, hallucinations, hangover effect, headache, hyperkinesia, impaired judgment, insomnia, nightmares, blood disorders, anxiety, hypoventilation, nausea, vomiting.

DDI:

Serious Griseofulvin activity reduces, Combined hormonal contraceptives causes bleeding & unintended pregnancies, Valproic acid causes excessive sedation & lethargy, Vit D/Calcium causes osteomalacia, Irinotecan clearance increases, Folic acid decreases drug level, Corticosteroids efficacy decreases, Coumarins efficacy reduces, Alcohol increases CNS depression (drowsiness, lack of alertness & impaired co-ordination), HIV protease inhibitors increases metabolism, Clozapine/Ciclosporin/Disopyramide/Efavirenz/Felodipine/Imatinib/Lamotrigine/Nevirapine/Nifedipine/Nimodipine/Verapamil level reduces, Carbamazepine levels increases, Theophylline reduces drug level Others Ifosfamide causes encephalopathy, Cefotaxime causes exanthematous skin reactions, Metronidazole/Chloramphenicol effects reduces, Felbamate increases adverse effects (drowsiness, lethargy, anorexia, ataxia), Mebendazole/Albendazole plasma levels reduces, Quinidine serum level reduces

Diet:

Monitor: Serum drug level, mental status, CBC, LFTs, seizure activity

PROMETHAZINE

Class:

SEDATING ANTI-HISTAMINE

ANTI-ALLERGIC, ANTI-EMETIC

SEDATIVE & HYPNOTIC

Pharmacokinetics :-

Absorption :Well absorbed

Distribution :Extensive

Metabolic :Hepatic

Excretion : Urine & bile

Indications & Dose:

ALLERGIC CONDITIONS/URTICARIA -

PO Adult 25mg HS or 12.5mg before meals & HS. Child >2 yr: 0.1mg/kg/dose, max 12.5mg q6h during day & 0.5mg/kg/dose max 25mg HS if needed

ANTIEMETIC

PO/IV/IM/RECTAL -

Adult 12.5-25mg q4-6h

Child 0.25-1mg/kg 4-6 times/day max 25mg/dose

HYPNOTIC ADJUNCT -

Combination therapy

IV/IM Adult 25-50mg with an analgesic or hypnotic Child >2 yr: 1.1mg/kgwith an analgesic or hypnotic at low dose.

MOTION SICKNESS -

Prophylactic therapy

PO/RECTAL -

Adult 25mg 30-60min before departure then q12h if needed Child 0.5mg/kg/dose 30-60min before departure then q12h if needed, max 25mg BID.

PRE/POSTOPERATIVE ANALGESIA

Combination therapy

IV/IM Adult 25-50mg with an analgesic or hypnotic Child >2 yr: 1.1mg/kgwith an analgesic or hypnotic at low dose.

SEDATION -

PO/IV/IM/RECTAL -

Adult 12.5-50mg/dose

Child 0.5-1mg/kg/dose q6h if needed, max 50mg/dose.

Contraindication :

Hypersensitivity, coma, asthma, LRTI treatment, children, intra-arterial/SC administration.

Precautions:

Bone marrow suppression, myasthenia gravis, glaucoma, parkinson's disease, respiratory disease, CVD, seizures, tranquilizers, prostatic hypertrophy, pyloroduodenal, barbiturates, general anesthesia

ADR:

Serious: bradycardia, hyper/hypotension, Nonspecific QT changes, postural hypotension, tinnitus, blurred vision, asthma, gynecomastia, thrombophlebitis, tissue necrosis, NMS, extrapyramidal symptoms, respiratory depression, impotence, amenorrhea,

Others: corneal & lenticular changes, urinary retention, blood disorders, urticaria, akathisia, confusion, delirium, disorientation, drowsiness, dystonia, euphoria, excitation, faintness, fatigue, hallucinations, insomnia, nightmares, dyskinesia, sedation, xerostomia, ejaculatory disorder, nausea, vomiting, nasal congestion, hyperglycemia.

DDI:

Serious Chloroquine (IM) level increases, CNS Depressants causes additive CNS depression, Pethidine increases respiratory depression, sedation, CNS toxicity & hypotension

Diet: With/without food

Monitor: Signs and symptoms of neuroleptic malignant syndrome, adverse CNS effects,CBC & LFT

TRICLOFOS

Class:

NON-BENZODIAZEPINE

SEDATIVE, HYPNOTIC

Indications & Dose:

INSOMNIA PO Adult 1-2g HS

Child <1 yr: 25-30mg/kg

1-5 yr: 250-500mg

6-12 yr: 0.5-1g

Contraindications :

CVD, gastritis, acute porphyria, prolonged use, abrupt withdrawal.

Precautions: Elderly, renal/hepatic impairment, history of alcohol/drug abuse

ADR:

Serious: Hypersensitivity reactions, SJS, erythema multiforme, ketonuria.

Others: abdominal distension, flatulence, drowsiness, light headedness, ataxia, hallucinations, nightmares, delirium, confusion, skin rashes, excitement.

ZALEPLON

Class:

NON-BENZODIAZEPINE

SEDATIVE, HYPNOTIC

Pharmacokinetics :

Absorption : Rapid & complete

Distribution : 1.4 L/kg (Vd)

Metabolic : Hepatic

Excretion :Urine (70%) & feces (17%)

Indications & Dose:

INSOMNIA Short-term therapy

PO Adult 10mg HS

Elderly 5mg HS

Contraindications :

Hypersensitivity, sleep apnea syndrome, myasthenia gravis, severe hepatic impairment, prolonged therapy.

Precautions:

Respiratory insufficiency, muscle weakness, history of drug/alcohol abuse, depression.

ADR:

Serious: Anaphylaxis, angioedema, complex sleep-related behaviour, hypersensitivity reactions, cholelithiasis, facial paralysis, ventricular tachycardia, hypo/hypertension, respiratory depression, urinary retention/incontinence, sedation.

Others: paradoxical excitation, visual disturbances, libido, GI disturbances, tremor, amnesia, drowsiness, muscle weakness, ataxia, vertigo, headache, confusion, depression, slurred speech, blood disorders, thrombophlebitis, dysarthria.

DDI:

Serious Phenobarbital/Carbamazepine/Phenytoin reduces drug efficacy Others Rifampicin decreases drug level, Alcohol enhances CNS depression, CNS Depressants increases CNS depression

ZOLPIDEM

Class:-

SELECTIVE BENZODIAZEPINE RECEPTOR AGONIST

SEDATIVE, HYPNOTIC

Pharmacokinetics :

Absorption :Rapid

Distribution : 0.54L/Kg (Vd)

Metabolic Hepatic

Excretion : Urine (48-67%), Feces (29-49%)

Indications & Dose:

INSOMNIA

PO- Adult IR tablet/sublingual

tablet/spray: 10mg HS max 10mg,

ER tablet: 12.5mg HS

Elderly IR tablet/sublingual tablet/spray: 5mg HS; ER tablet: 6.25mg HS

Contraindications :

Hypersensitivity to zolpidem, obstructive sleep apnea, acute/severe respiratory depression, myasthenia gravis, severe hepatic impairment, psychotic illness, long-term therapy

Precautions: Depression, muscle weakness, history of drug /alcohol abuse, renal impairment, elderly

ADR:

Serious: Chest discomfort/pain, palpitation, arthritis, bronchitis, arthralgia, urticaria, CVD, hepatic function abnormalities, hyper/hypotension, leukopenia, lymphadenopathy, migraine, tongue paresthesia, ARF, vaginitis, tachycardia, anaphylaxis, angioedema, complex sleep-related behavior, UTI, thrombosis, menstrual disorder, visual disturbance, urinary incontinence, Others: Anemia, rash, abnormal dreams, anxiety, myalgia, abdominal pain, constipation, nausea, vomiting, URTIs.

DDI: Serious CNS Depressants/Alcohol increases CNS depressant effects of drug, Ritonavir increases drug level Others Rifampicin/Alcohol decreases drug level

Diet: After food

Monitor: Daytime alertness, respiratory rate, behavior profile, LFTs

ZOPICLONE

Class:-

NON-BENZODIAZEPINE

HYPNOTIC

Pharmacokinetics :

Absorption : Rapid

Distribution : Extensive

Metabolism : Hepatic

Excretion : Urine (5%)& feces (16%)

Indications & Dose:

INSOMNIA

Short-term therapy

PO Adult 7.5mg HS

Elderly 3.75mg HS

Contraindications :

Hypersensitivity to drug, myasthenia gravis, respiratory failure, severe sleep apnea syndrome, long-term therapy.

Precautions:

Elderly, muscle weakness, history of drug abuse, psychiatric illness, hepatic/renal impairment, depression, drug abuse/alcoholism, abrupt withdrawal.

ADR:

Serious: Hypersensitivity reactions, sedation, depression, paradoxical excitation, respiratory depression, hypotension, disinhibition, jaundice, blood disorders, urinary retention/incontinence, visual disturbances, Others: GI disturbances, bitter or metallic taste, Headache, drowsiness, muscle weakness, ataxia, vertigo, confusion, slurred speech, libido, tremor.

DDI:

Others Ketoconazole/Itraconazole increases drug level, Rifampicin reduces drug level.

Diet: After food (just before bedtime)

Monitor: LFTs, excessive drowsiness (in elders