Haloperidol

Indication & Dosage

Psychoses

Adult: 0.5-5 mg bid/tid, may increase up to 100 mg daily in severe or resistant cases.
Usual maintenance: 3-10 mg daily.

Restlessness and confusion

Adult: 1-3 mg every 8 hr.

Acute psychosis

Adult: Doses range from 2-10 mg, may be given every hr or at intervals of 4-8 hr,
until symptoms are controlled. Max: 18 mg/day. For emergency control of severely
disturbed patients: Up to 18 mg may be given IV/IM.

Administration

May be taken with or without food. (May be taken w/ meals to minimise GI irritation.)

Contraindications

Severe toxic CNS depression; preexisting coma; Parkinson's disease; lactation.

Special Precautions

Parkinsonism; epilepsy, allergy, angle-closure glaucoma, benign prostatic

hyperplasia; severe cardiac or hepatic disease; extremes in temp (hot and cold
weather); presence of acute infections or leucopenia; hyperthyroidism; pregnancy,
elderly, children. Patients receiving anticoagulants. Discontinue upon signs of
neurological toxicity in patients taking haloperidol and lithium.

Adverse Drug Reactions

Tardive dyskinesia; extrapyramidal reactions. Anxiety, drowsiness, depression,

anorexia, transient tachycardia, postural hypotension, leukopenia; anticholinergic
side effects.

Potentially Fatal: Neuroleptic malignant syndrome.

Mechanism of Action

Haloperidol blocks postsynaptic dopamine D1 and D2 receptors in the mesolimbic

system and decreases the release of hypothalamic and hypophyseal hormones. It
produces calmness and reduces aggressiveness with disappearance of hallucinations
and delusions

MIMS Class

Antipsychotics / Antivertigo Drugs

ATC Classification

N05AD01 - haloperidol; Belongs to the class of butyrophenone derivatives

antipsychotics. Used in the management of psychosis.
Fluphenazine decanoate

Indication & Dosage

Oral

Psychoses

Adult: Initially, 2.5-10 mg daily in 2-3 divided doses, increased according to reponse.
Maintenance: 1-5 mg daily.

Max Dosage: Adult: 20 mg/day. Elderly: 10 mg/day.

Oral

Mania

Adult: Initially, 2.5-10 mg daily in 2-3 divided doses, increased according to reponse.
Maintenance: 1-5 mg daily.

Max Dosage: Adult: 20 mg/day. Elderly: 10 mg/day.

Oral

Schizophrenia

Adult: Initially, 2.5-10 mg daily in 2-3 divided doses, increased according to reponse.
Maintenance: 1-5 mg daily.

Max Dosage: Adult: 20 mg/day. Elderly: 10 mg/day.

Oral

Short-term adjunct in severe anxiety or behavioral disturbances

Adult: 1 mg bid increased to 2 mg bid if necessary.

Intramuscular

Psychoses

Adult: As decanoate: Initially, 12.5 mg adjusted according to response. Maintenance:

12.5-100 mg at intervals of 2-6 wk. For doses >50 mg, increments should be made
slowly in steps of 12.5 mg. The enantate ester can be given in similar doses at
intervals of 1-3 wk.

Elderly: 6.25 mg adjusted according to response.

Intramuscular

Mania

Adult: As decanoate: Initially, 12.5 mg adjusted according to response. Maintenance:

12.5-100 mg at intervals of 2-6 wk. For doses >50 mg, increments should be made
slowly in steps of 12.5 mg. The enantate ester can be given in similar doses at
intervals of 1-3 wk.
Elderly: 6.25 mg adjusted according to response.

Intramuscular

Schizophrenia

Adult: As decanoate: Initially, 12.5 mg adjusted according to response. Maintenance:

12.5-100 mg at intervals of 2-6 wk. For doses >50 mg, increments should be made
slowly in steps of 12.5 mg. The enantate ester can be given in similar doses at
intervals of 1-3 wk.

Elderly: 6.25 mg adjusted according to response.

Administration

May be taken with or without food.

Contraindications

Hypersensitivity; comatose or severely depressed states; blood dyscrasias; liver

disease; bone marrow depression; phaeochromocytoma; suspected or established
subcortical brain damage with or without hypothalamic damage; pregnancy (3rd
trimester), lactation.

Special Precautions

Presence of convulsive disorders; hepatic, renal, cerebrovascular, resp and CV

diseases; elderly or debilitated patients. May elevate prolactin levels which may
persist after chronic admin. May exacerbate depression. Closed-angle glaucoma.
History of jaundice, parkinsonism, DM, hypothyroidism, myasthenia gravis, paralytic
ileus, prostatic hyperplasia or urinary retention. Regular eye examinations in patients
receiving long term therapy. Avoid direct sunlight exposure.

Adverse Drug Reactions

Tardive dyskinesia, sedation, mental confusion; hypotension; hyperprolactinaemia

leading to galactorrhoea and amenorrhoea in women; loss of libido, impotence and
sterility in males. Allergic reactions, cholestatic jaundice, corneal and lens deposits,
skin pigmentation.

Potentially Fatal: Agranulocytosis; neuroleptic malignant syndrome.

Drug Interactions

Reduces antihypertensive effects of guanethidine, methyldopa and clonidine. Lithium

toxicity. Reduced bioavailability with antacids. Increased risk of arrhythmia when
used with drugs that prolong QT interval. May cause electrolyte disturbance when
used with diuretics.

Potentially Fatal: Additive CNS depressant effects with alcohol, barbiturates,

hypnotics, sedatives, opiates and antihistamines.

Mechanism of Action

Fluphenazine blocks postsynaptic dopamine D1 and D2 receptors in the mesolimbic

system and decreases the release of hypothalamic and hypophyseal hormones. It
reduces aggressiveness with disappearance of hallucinations and delusions.
Onset: 1-3 days.

Duration: 2-4 days.

MIMS Class

Antipsychotics

ATC Classification

N05AB02 - fluphenazine; Belongs to the class of phenothiazine antipsychotics with

piperazine structure. Used in the management of psychosis.

Biperiden

Indications

Tab Adjunct therapy of all forms of parkinsonism (post-encephalatic, arteriosclerotic

& idiopathic). Amp Symptomatic treatment of parkinsonism including the alleviation
of the extrapyramidal syndrome induced by drugs.

Dosage

Tab Adult Parkinsonism Initially 1 mg bid, increased by 2 mg/day. Max: 16 mg daily.

Drug-induced movement disorders 1-4 mg once-qid. Childn 3-15 yr 1-2 mg once-tid.

Administration

Should be taken with food

Contraindications

Untreated narrow-angle glaucoma, intestinal stenoses or obstruction, megacolon,

prostatic hypertrophy, life-threatening tachycardia.

Special Precautions

Avoid abrupt discontinuation, increased sensitivity to side effects esp elderly;

enhanced risk of cerebral seizures in predisposed persons, abuse, impaired ability to
drive or operate machinery.

Adverse Drug Reactions

Fatigue, dizziness, drowsiness, dry mouth, rarely, swelling of salivary glands,

accommodation difficulties, mydriasis & photophobia, hypohydrosis, constipation,
gastric symptoms, nausea, tachycardia, very rarely, bradycardia, esp at higher
doses, restlessness, agitation, anxiety, confusion, euphoria, occasionally, impairment
of memory, in rare cases, delirium, hallucinations, nervousness, headache, insomnia,
dyskinesia, ataxia, muscle twitching, speech impairment.

Drug Interactions

Enhanced anticholinergic effects in combination w/ other psychotropic drugs,

antihistamines, antiparkinsonism drugs, antispasmodics, quinidine & pethidine.
Dyskinesia induced by levodopa may be potentiated. Effects of alcohol may be
enhanced. Antagonistic influence on the action of metoclopramide & compd of similar
activity in the GIT.

MIMS Class

Antiparkinsonian Drugs

ATC Classification

N04AA02 - Biperiden ; Belongs to the class of tertiary amines anticholinergic agents.

Used in the management of Parkinson's disease.

Chlorpromazine

Indication Dosage

Psychoses 25 mg 3 times/day. Maintenance: 25-100 mg 3 times/day, increased to ≥1

g/day if needed in psychotic patients. IM Psychoses 25-50 mg 6-8 hrly.

Overdosage

Symptoms include somnolence, coma, hypotension and extrapyramidal symptoms.

Other possible manifestations include agitation and restlessness, convulsions, fever,
autonomic reactions such as dry mouth and ileus, EKG changes and cardiac
arrhythmias. Treatment is symptomatic and supportive. Early gastric lavage may be
helpful. Observe patient and maintain an open airway.

Contraindications

Hypersensitivity; preexisting CNS depression, coma, bone-marrow supression;

phaeochromocytoma; lactation.

Special Precautions

Parkinson's disease; CV disease; renal or hepatic impairment; cerebrovascular and

respiratoty disease; jaundice; DM; hypothyroidism; paralytic ileus; prostatic
hyperplasia or urinary retention; epilepsy or history of seizures; myasthenia gravis;
pregnancy; elderly (especially with dementia), and debilitated patients. Avoid direct
sunlight.

Adverse Drug Reactions

Tardive dyskinesia (on long-term therapy). Involuntary movements of extremities

may also occur. Dry mouth, constipation, urinary retention, mydriasis, agitation,
insomnia, depression and convulsions; postural hypotension, ECG changes. Allergic
skin reaction, amenorrhoea, gynaecomastia, weight gain. Hyperglycaemia and raised
serum cholesterol.

Potentially Fatal: Agranulocytosis. Instantaneous deaths associated with ventricular

tachyarrhythmias. Marked elevation of body temperature with heat stroke.
Neuroleptic malignant syndrome, extrapyramidal dysfunction.

Drug Interactions

Potentiation of anticholinergic effects of antiparkinson agents and TCAs may lead to

an anticholinergic crisis. Additive orthostatic hypotensive effect in combination with
MAOIs. Reverses antihypertensive effect of guanethidine, methyldopa and clonidine.
Potentially Fatal: Additive depressant effect with sedatives, hypnotics,
antihistamines, general anaesthetics, opiates and alcohol.

Mechanism of Action

Chlorpromazine is a neuroleptic that acts by blocking the postsynaptic dopamine

receptor in the mesolimbic dopaminergic system and inhibits the release of
hypothalamic and hypophyseal hormones. It has antiemetic, serotonin-blocking, and
weak antihistaminic properties and slight ganglion-blocking activity.

Onset: 15 min (IM); 30-60 min (oral)

MIMS Class

Antipsychotics / Antiemetics

ATC Classification

N05AA01 - chlorpromazine; Belongs to the class of phenothiazine antipsychotics with

aliphatic side-chain. Used in the management of psychosis.

Levomepromazine

Indication Dosage

Adult: PO Schizophrenia As maleate: 25-50/day in 3 divided doses, w/ higher dose at

night. Non-ambulant: 100-200 mg/day. Max: 1g/day.

Contraindications

Comatose state, severe CNS depression, phaeochromocytoma, blood dyscrasia.

Special Precautions

Reduced GI motility, urinary retention, prostatic hyperplasia, xerostomia or visual

problems, narrow-angle glaucoma, myasthenia gravis. Cardiac conduction
abnormalities. Patients at risk of hypotension or CV or cerebrovascular disease. Bone
marrow suppression. Severe renal, cardiac or hepatic disease. Respiratory disease.
Predisposition to seizures. May affect driving, especially at start of treatment. Elderly,
children. Pregnancy and lactation.

Adverse Drug Reactions

Hypotension, orthostatic hypotension, tachycardia, QT prolongation; photosensitivity,

rash; gynaecomastia, wt gain, irregular menstruation, changes in libido;
extrapyramidal effects, dizziness, seizure, headache, drowsiness, neuroleptic
malignant syndrome, interference with temperature regulation; constipation, nausea,
vomiting, ileus; urinary retention, ejaculatory disorders, incontinence, polyuria,
priapism; blood dyscrasias; jaundice, hepatotoxicity.

Potentially Fatal: Arrhythmias. Severe orthostatic hypotension.

Drug Interactions

Increased risk of extrapyramidal effects with metoclopramide, acetylcholinesterase

inhibitors. Additive hypotensive effects with antihypertensive agents, trazodone.
Additive sedative effects with CNS depressants. May alter levels/effects of CYP2D6
substrates and prodrug substrates. Reduced pressor effects of epinephrine. Reduced
effects of bromocriptine, guanethidine, guanadrel, levodopa. Increased neurotoxicity
with lithium (rare). Reduced serum levels with phenytoin or increased phenytoin
toxicity. Increased serum concentrations with propranolol, sulfadoxine-
pyrimethamine. Increased serum levels of valproic acid. Reduced absorption with
aluminium salts. Reduced effects of amphetamines or increased risk of psychotic
symptoms. Reduced effects and excessive anticholinergic effects with benztropine,
trihexyphenidyl, biperiden, TCAs, antihistamines, disopyramide.

Potentially Fatal: Increased risk of ventricular arrhythmias with drugs that

prolong the QT interval. Increased toxicity with MAOIs.

Mechanism of Action

Levomepromazine is a phenothiazine with CNS depressant, α-adrenergic-blocking,

antimuscarinic, antihistaminic and analgesic activity. It acts by blocking dopamine
receptors in the mesolimbic dopaminergic system.

Onset: 1 hr (parenteral).

Duration: 2-4 hr (parenteral).

MIMS Class

Antipsychotics / Antivertigo Drugs / Analgesics (Non-Opioid) & Antipyretics

ATC Classification

N05AA02 - levomepromazine; Belongs to the class of phenothiazine antipsychotics

with aliphatic side-chain. Used in the management of psychosis.

Lithium carbonate

Dosage

Adult: PO Bipolar disorder; Mania; Recurrent unipolar depression Dose depends on

the preparation used. Adjust doses to produce a serum-lithium concentration of 0.4-1
mmol/L.

Administration

Should be taken with food.

Contraindications

Severe renal and cardiac disease; severe dehydration, sodium depletion, debilitation.

Special Precautions

Monitor serum lithium levels (twice wkly or more frequently in acute phase; at least
every 2 mth during maintenance). Thyroid disorders, mild to moderate renal or
cardiac impairment. Marked fluid loss (protracted sweating, diarrhoea or prolonged
fever). Maintain normal fluid and salt intake. Elderly. Monitor changes in renal
function. Patients with suicidal tendency. May impair ability to drive or operate
machinery. Children <12 yr. Pregnancy and lactation.
Adverse Drug Reactions

Exacerbation of psoriasis, acne, rash; nausea, diarrhoea, vertigo, muscle weakness,

dazed feeling; loss of concentration; tremors; hypothyroidism; wt gain, oedema;
cardiac arrhythmias; exophthalmos; restlessness; electrolyte disturbances.

Potentially Fatal: Severe neurotoxicity, leucopenia.

Drug Interactions

Reduced serum levels with carbonic anhydrase inhibitors, chlorpromazine, sodium-

containing preparations, theophylline, urea. Enhanced hypothyroid effects with iodine
salts. Enhanced effects of neuromuscular-blocking agents. Reduced pressor response
to sympathomimetics.

Potentially Fatal: Increased risk of lithium toxicity with ACE inhibitors, angiotensin
receptor antagonists, loop diuretics, metronidazole, phenytoin. Increased risk of
neurotoxicity with carbamazepine, calcium-channel blockers, haloperidol,
methyldopa, phenothiazines, SSRIs, TCAs. Increased serum levels with COX-2
inhibitors, NSAIDs (except sulindac, aspirin), tetracyclines, thiazide diuretics.
Increased risk of encephalopathy with haloperidol. Increased risk of serotonin
syndrome with sibutramine. Fatal malignant hyperpyrexia may occur when used with
MAOIs.

Food Interaction

Caffeine may reduce serum concentrations of lithium.

Mechanism of Action

Lithium's exact mechanism is unclear but it alters intraneuronal metabolism of

catecholamines and sodium transport in neurons and muscle cells.

Absorption: Readily and completely absorbed from the GI tract (oral); serum levels
increase with food. Peak plasma concentrations after 0.5-3 hr (conventional
preparation), 2-12 hr (modified-release preparations).

MIMS Class

Antidepressants

ATC Classification

N05AN - Lithium; Used in the management of psychosis.

N05AN01 - lithium; Belongs to the class of lithium antipsychotics. Used in the

management of psychosis.

Risperidone

Indications

Treatment of acute & chronic psychoses.

Dosage
Schizophrenia Adult Start w/ 2 mg/day. Dosage may be increased on the 2nd day to 4
mg. Most patients will benefit from daily doses of 4-6 mg. Dosage can be maintained
unchanged or further individualized. Benzodiazepine may be added when additional
sedation is required. Elderly Start at 0.5 mg bid & titrate up to 1-2 mg bid in
increments of 0.5 mg/day.

Administration

May be taken with or without food (Place on the tongue & allow to disintegrate. May
then be swallowed w/ or without water.).

Special Precautions

Elderly w/ dementia. Known CV disease, dosage should be gradually titrated as

recommended, a dose reduction should be considered when hypotension occurs.
Monitor for signs of tardive dyskinesia. Neuroleptic malignant syndrome.
Extrapyramidal symptoms. Hyperglycemia, epilepsy, wt gain. Renal or liver
insufficiency. Driving/operating machinery. Pregnancy & lactation.

Adverse Drug Reactions

Insomnia, agitation, anxiety, headache, somnolence, fatigue, dizziness, impaired

conc, constipation, dyspepsia, nausea, vomiting, abdominal pain, blurred vision,
priapism, erectile, ejaculatory & orgastic dysfunction, urinary incontinence,
angioedema, rhinitis, rash & allergic reactions. Occasionally, (orthostatic)
hypotension, (reflex) tachycardia or HTN. Extrapyramidal symptoms, wt gain. Dose-
dependent increase in plasma prolactin conc, water intoxication. CVA &
hyperglycemia.

Drug Interactions

Levodopa & other dopamine agonists. Carbamazepine or other hepatic enzyme

inducer. Phenothiazines, tricyclic depressants & some β-blockers. Fluoxetine,
paroxetine, furosemide, cimetidine & ranitidine.

MIMS Class

Antipsychotics

ATC Classification

N05AX08 - Risperidone ; Belongs to the class of other antipsychotics.

Clozapine

Dosage

Adult: PO Schizophrenia 12.5 mg 1-2 times on day 1, followed by 25 mg 1-2 times on

day 2. Increase gradually according to response. Usual range: 200-450 mg/day. Max:
900 mg/day. Psychoses in Parkinson's disease Initial: 12.5 mg/day at night, increase
gradually. Usual range: 25-37.5 mg/day. Max: 100 mg/day.

Administration

May be taken with or without food.

Contraindications

History of bone marrow disorders including agranulocytosis, circulatory collapse,

alcoholic or toxic psychosis, drug intoxication, uncontrolled epilepsy, severe renal,
hepatic or cardiac disease; paralytic ileus. Pregnancy and lactation.

Special Precautions

Leucocyte counts should be monitored regularly and for at least 4 wk after treatment
discontinuation. Renal, hepatic or cardiac impairment; prostatic enlargement,
narrow-angle glaucoma; elderly; immobilised patients

Adverse Drug Reactions

Drowsiness, dizziness, headache; nausea, vomiting, constipation; anxiety, confusion,

fatigue, transient fever. Rarely, dysphagia, acute pancreatitis, cholestatic jaundice;
orthostatic hypotension, tachycardia; seizures; hypersalivation.

Potentially Fatal: Rarely, thromboembolism. Reversible neutropenia which

may progress to a potentially fatal agranulocytosis. Fatal myocarditis.

Drug Interactions

Reduced plasma concentrations with concomitant use of phenytoin. May enhance the
central effects of MAOIs.

Potentially Fatal: Concurrent use with bone marrow suppressants e.g.

carbamazepine, co-trimoxazole, chloramphenicol, penicillamine,
sulfonamides, antineoplastics or pyrazolone analgesics; long-acting depot
antipsychotics.

Mechanism of Action

Clozapine has relatively weak dopamine receptor-blocking activity at D1, D2, D3 and
D5 receptors but has high affinity for the D4 receptor. It has also blocking effects on
serotonin, α-adrenergic histamine H1 and cholinergic receptors.

Absorption: Absorbed well from the GI tract (oral); peak plasma concentrations after
2.5 hr.

MIMS Class

Antipsychotics

ATC Classification

N05AH02 - clozapine; Belongs to the class of diazepines, oxazepines and thiazepines

antipsychotics. Used in the management of psychosis.

Divalproex sodium

Dosage

Adult: PO Partial seizures; Primary generalised seizures Initial: 10-15 mg/kg/day in 2-

4 divided doses. Max: 60 mg/kg/day. Acute manic episodes of bipolar disorder Initial:
25 mg/kg once daily. Max: 60 mg/kg/day.
Administration

Should be taken with food.

Contraindications

Hepatic disease or severe hepatic impairment; porphyria. Pregnancy.

Special Precautions

Children <2 yr; congenital metabolic disorders; organic brain disease or severe
seizure disorders; HIV infection; renal impairment; lactation. Monitor liver function
before and during the 1st 6 mth of therapy. Monitor platelet function, signs of
pancreatitis and SLE. Gradual withdrawal of valproate. May impair ability to drive or
operate machinery. Increased risk of hyperammonaemic encephalopathy in patients
with urea cycle disorders.

Adverse Drug Reactions

Behavioural/mood changes; hyperammonaemia; pancreatitis, thrombocytopenia.

Abdominal cramps, anorexia, diarrhoea, hair loss, indigestion, nausea and vomiting;
tremor; unusual weight loss or gain.

Potentially Fatal: Hepatic failure, pancreatitis.

Drug Interactions

Felbamate increases valproate levels. Phenytoin, phenobarbitone and carbamazepine

lower valproate levels. Increased risk of hepatotoxity with hepatotoxic drugs.

Potentially Fatal: Potentiates action of CNS depressants (barbiturates,

primidone) and alcohol.

Food Interaction

Food may delay the extent of absorption. Divalproex may cause GI upset; take with
large amount of water of food to decrease GI upset.

Mechanism of Action

Divalproex sodium dissociates to the valproate ion in the GI tract. It is thought to

work by increasing brain concentrations of GABA which may also play an important
role in the prevention of migraine attacks.

Distribution: Plasma protein binding ranges from 10-18.5%.

Metabolism: Almost entirely by liver.

MIMS Class

Antipsychotics / Antimigraine Preparations / Anticonvulsants

Lamotrigine

Dosage
 Bipolar disorder Monotherapy: Initial : 25 mg once daily for 2 wk, increase gradually
to maintenance dose: 200 mg/day. W/ valproate: Initial: 25 mg every other day for 2
wk, increase gradually to maintenance: 100 mg/day. W/ enzyme-inducing drugs
(except valproate): Initial: 50 mg once daily for 2 wk, then increase gradually to
maintenance: 400 mg/day in 2 divided doses.

Administration

May be taken with or without food.

Special Precautions

Hepatic or renal impairment. Closely monitor patient. Monitor children's body wt.
Advise patient to report any hypersensitivity reaction. Avoid abrupt withdrawal unless
severe skin reactions have developed. May impair ability to drive or operate
machinery. Pregnancy and lactation.

Adverse Drug Reactions

Skin eruptions usually maculopapular in nature, nausea, headache, tiredness,

dizziness, ataxia, irritability/aggression, tremor, agitation, confusion, hallucination,
diplopia, blurred vision. Haematological abnormalities e.g. leucopenia and
thrombocytopenia. Elevations of LFTs. Arthralgia, pain and back pain.

Potentially Fatal: Stevens-Johnson syndrome and toxic epidermal

necrolysis.

Drug Interactions

Metabolism enhanced by enzyme-inducing drugs e.g. phenytoin, carbamazepine,

phenobarbitone, primidone, rifampicin, ethinyloestradiol/levonorgestrel combination.
Metabolism reduced by sodium valproate.

Mechanism of Action

Lamotrigine inhibits voltage-sensitive sodium channels, thereby stabilising neuronal

membranes and consequently inhibiting pathological release of excitatory amino
acids (e.g. glutamate and aspartate). These amino acids play a role in the generation
and spread of epileptic seizures.

Absorption: Well absorbed from the GI tract (oral); peak plasma concentrations after
2.5 hr.

MIMS Class

Anticonvulsants / Antipsychotics

ATC Classification

N03AX09 - lamotrigine; Belongs to the class of other antiepileptics. Used in the

management of epilepsy.

Clonazepam

Dosage
Panic disorder

Adult: Initially, 250 mcg bid, increased after 3 days up to 1 mg daily. Max: 4 mg daily.

Hepatic impairment: Dose reduction may be needed.

Administration

May be taken with or without food.

Contraindications

Hypersensitivity to benzodiazepines, acute pulmonary insufficiency, acute narrow

angle glaucoma.

Special Precautions

Neonates, chronic pulmonary insufficiency, hepatic/renal dysfunction, porphyria,

elderly; pregnancy and lactation.

Adverse Drug Reactions

Drowsiness, fatigue, muscular hypotonia, coordination disturbances, dizziness,

vertigo, anorexia, visual disturbances, libido changes.

Potentially Fatal: Salivary or bronchial hypersecretion leading to respiratory problems

(children). May produce diminished reflexes or coma. Rarely, blood dyscrasias.

Drug Interactions

Carbamazepine, phenobarbitone or phenytoin may accelerate clonazepam

metabolism.

Potentially Fatal: Increased sedative effect with alcohol, general anaesthetics and
TCAs.

Mechanism of Action

Clonazepam is an effective anticonvulsant. It raises the threshold for propagation of

seizure activity and prevents generalisation of focal or local activity. Clinically, it
improves focal epilepsy and generalised seizures. It is also believed to enhance the
activity of GABA, and acts as anxiolytic.

Absorption: Well absorbed from the GI tract (oral); peak plasma concentrations after
4 hr.

MIMS Class

Anxiolytics / Anticonvulsants

ATC Classification

N03AE01 - clonazepam; Belongs to the class of benzodiazepine derivatives

antiepileptic. Used in the management of epilepsy.

Lamotrigine
Dosage

Bipolar disorder Monotherapy: Initial : 25 mg once daily for 2 wk, increase gradually
to maintenance dose: 200 mg/day. W/ valproate: Initial: 25 mg every other day for 2
wk, increase gradually to maintenance: 100 mg/day. W/ enzyme-inducing drugs
(except valproate): Initial: 50 mg once daily for 2 wk, then increase gradually to
maintenance: 400 mg/day in 2 divided doses.

Administration

May be taken with or without food.

Special Precautions

Hepatic or renal impairment. Closely monitor patient. Monitor children's body wt.
Advise patient to report any hypersensitivity reaction. Avoid abrupt withdrawal unless
severe skin reactions have developed. May impair ability to drive or operate
machinery. Pregnancy and lactation.

Adverse Drug Reactions

Skin eruptions usually maculopapular in nature, nausea, headache, tiredness,

dizziness, ataxia, irritability/aggression, tremor, agitation, confusion, hallucination,
diplopia, blurred vision. Haematological abnormalities e.g. leucopenia and
thrombocytopenia. Elevations of LFTs. Arthralgia, pain and back pain.

Potentially Fatal: Stevens-Johnson syndrome and toxic epidermal

necrolysis.

Drug Interactions

Metabolism enhanced by enzyme-inducing drugs e.g. phenytoin, carbamazepine,

phenobarbitone, primidone, rifampicin, ethinyloestradiol/levonorgestrel combination.
Metabolism reduced by sodium valproate.

Mechanism of Action

Lamotrigine inhibits voltage-sensitive sodium channels, thereby stabilising neuronal

membranes and consequently inhibiting pathological release of excitatory amino
acids (e.g. glutamate and aspartate). These amino acids play a role in the generation
and spread of epileptic seizures.

Absorption: Well absorbed from the GI tract (oral); peak plasma concentrations after
2.5 hr.

MIMS Class

Anticonvulsants / Antipsychotics

ATC Classification

N03AX09 - lamotrigine; Belongs to the class of other antiepileptics. Used in the

management of epilepsy.

Quetiapine
Dosage

Adult: PO Schizophrenia Initial: 25 mg twice daily on day 1, increase to 50 mg twice

daily on day 2, 100 mg twice daily on day 3 and 150 mg twice daily on day 4. Usual:
300-450 mg/day. Max: 750 mg/day. Bipolar disorder Manic phase: 50 mg twice daily,
increase by 50 mg/dose for each subsequent day till 3rd day. Usual: 400-800 mg/day.
Increase slowly if needed. Depressive phase: Initial: 50 mg at bedtime on day 1, 100
mg on day 2, 200 mg on day 3, and 300 mg on day 4. May increase to 400 mg on
day 5 and 600 mg on day 8 if needed.

Administration

May be taken with or without food.

Contraindications

Severe CNS depression, bone marrow suppression, coma.

Special Precautions

CV disease, cerebrovascular disease or conditions that predispose to hypotension.

History of seizures; neuroleptic malignant syndrome; tardive dyskinesia. Monitor
glycaemic control, especially in diabetics. Hepatic or renal impairment. Gradual
withdrawal is recommended. Monitor for signs of clinical worsening, suicidality or
unusual changes in behaviour. Pregnancy and lactation.

Adverse Drug Reactions

Headache, asthenia, abdominal pain, back pain, fever, chest pain, postural and
orthostatic hypotension, hypertension, constipation, dry mouth, dyspepsia, diarrhoea,
leucopenia, elevations in serum transaminase level, weight gain, myalgia,
somnolence, dizziness, anxiety, rhinitis, rash, dry skin, ear pain, UTI, syncope,
neuroleptic malignant syndrome, variations in WBC count, neutropenia, eosinophilia,
elevations in nonfasting serum triglyceride level and total cholesterol, decrease in
thyroid hormone levels, prolongation of the QTc interval.

Drug Interactions

Increased risk of drowsiness and postural hypotension when used with alcohol.
CYP3A4 inducers eg. phenytoin and carbamazepine may decrease plasma levels of
quetiapine while CYP3A4 inhibitors eg. ketoconazole and erythromycin may increase
its plasma levels.

Mechanism of Action

Quetiapine is an antagonist at multiple neurotransmitter receptors in the brain:

Serotonin 5-HT1A and 5-HT2, dopamine D1 and D2, histamine H1 and adrenergic a1
and a2 receptors. It is used in the treatment of schizophrenia and bipolar disorder.

Absorption: Well absorbed after oral doses.

MIMS Class

Antipsychotics

ATC Classification

N05AH04 - quetiapine; Belongs to the class of diazepines, oxazepines and

thiazepines antipsychotics. Used in the management of psychosis.

Demerol

Contents

Pethidine HCl

Indications

Relief of moderate to severe pain, pre-op medication, support of anesth & obstet
analgesia.

Dosage

Pain relief Adult 50-150 mg. Childn 0.5-0.8 mg/lb. To be given 3-4 hrly by IM or SC inj.
Pre-op medication Adult 50-100 mg. Childn 0.5-1 mg/lb. To be given IM or SC 30-90
mins before start of anesth. Support of anesth Repeated slow IV inj of fractional
doses eg 10 mg/mL or continue IV infusion of a more diluted soln eg 1 mg/mL. Obstet
analgesia 50-100 mg IM or SC when pain becomes regular; may be repeated at 1-3
hrly.

Special Precautions

Head injury, increased intracranial pressure, acute asthma & other resp conditions,
atrial flutter & other supraventricular tachycardias, convulsive disorders, acute
abdominal conditions. Severe impairment of hepatic or renal function, debilitated,
hypothyroidism. Addison's disease & prostatic hypertrophy or urethral stricture. >65
yr. May impair ability to drive or operate machinery.

Adverse Drug Reactions

Resp depression, circulatory depression, resp arrest, shock, cardiac arrest. GI

disturbance. Lightheadedness, dizziness, sedation, nausea, vomiting, sweating.
Euphoria, dysphoria, weakness, headache, tremor, agitation, uncoordinated muscle
movements, severe convulsions, transient hallucinations & disorientation, visual
disturbance. Flushing, tachycardia, bradycardia, palpitation, hypotension, syncope,
phlebitis. Urinary retention. Allergic reactions. Pain at inj site, local tissue irritation.

Drug Interactions

Other narcotic analgesics, general anesth, phenothiazines, tranquillizers, sedative-

hypnotics, tricyclic antidepressants, MAOIs & other CNS depressants (including
alcohol).

MIMS Class

Anaesthetics - Local & General / Analgesics (Opioid)

ATC Classification

N02AB02 - Pethidine ; Belongs to the class of phenylpiperidine derivative opioids.

Used to relieve pain.
Olanzapine

Dosage

Adult: PO Schizophrenia Initial: 5-10 mg/day adjust according to response. Usual: 5-

20 mg/day. Max: 20 mg/day. Acute mixed or manic episodes in bipolar disorder
Initial: 10 or 15 mg/day as monotherapy or 10 mg/day as part of combination
therapy. Usual: 5-20 mg/day. For prevention of recurrence: Start w/ 10 mg/day. IM
Rapid control of agitation and disturbed behaviour in schizophrenia or mania Initial:
5-10 mg, followed by 5-10 mg 2 hr later if needed. Max: 3 inj per 24-hr period; Max
(including oral doses): 20 mg/day. Max duration: 3 days; transfer to oral therapy as
soon as possible.

Administration

May be taken with or without food.

Contraindications

Angle-closure glaucoma; lactation. IM: History of CVS disease, heart surgery.

Special Precautions

Impaired renal, hepatic, cardiovascular function; prostatic hypertrophy; paralytic

ileus; DM; parkinsonism; pregnancy. History of blood dyscrasias, myelosuppression,
seizures; dementia; dyslipidaemia. IM: Hypotension, bradyarrhythmia,
hypoventilation; monitor BP carefully. Caution when used in adolescents due to
increased risk of weight gain and hyperlipidaemia. Efficacy and safety have not been
established in paediatric patients <13 yr.

Adverse Drug Reactions

Postural hypotension; constipation; dizziness; wt gain; agitation; insomnia; akathisia;

tremor; personality disorders; oedema; somnolence; increased appetite;
antimuscarinic effects; speech difficulty; exacerbation of Parkinson's disease;
hallucinations; asthenia; increased body temperature; bradycardia;
hyperprolactinaemia; QT prolongation (uncommon); asymptomatic elevations of
hepatic transaminases.

Potentially Fatal: Exacerbation of preexisting diabetes sometimes leading

to ketoacidosis. Neuroleptic malignant syndrome.

Drug Interactions

Olanzapine may antagonise the effects of levodopa and dopamine agonists. Drugs
that induce CYP1A2 or glucuronyl transferase enzymes e.g. omeprazole and
rifampicin, may increase olanzapine clearance. Inhibitors of CYP1A2 may potentially
inhibit olanzapine elimination. Carbamazepine may increase the clearance of
olanzapine. Concomitant admin of activated charcoal reduced the oral bioavailability
of olanzapine by 50-60%. Caution should be taken when olanzapine is administered
with centrally acting drugs and alcohol.

Mechanism of Action

Olanzapine is an atypical antipsychotic with affinity for serotonin 5-HT2A/2C,

dopamine, muscarinic M1-M5, histamine H1 and adrenergic α1 receptors.
Absorption: Well absorbed from the GI tract (oral); peak plasma concentrations after
5-8 hr (oral) or 15-45 min (IM).

MIMS Class

Antipsychotics

ATC Classification

N05AH03 - olanzapine; Belongs to the class of diazepines, oxazepines and

thiazepines antipsychotics. Used in the management of psychosis.

Essentiale forte

Contents

Per Essentiale cap Nicotinamide 15 mg, 3-SN- phosphatidyl choline 175 mg, vit B1 3
mg, vit B12 3 mcg, vit B2 3 mg, vit B6 3 mg, vit E acetate 3.3 mg. Per Essentiale
Forte cap Nicotinamide 30 mg, 3-SN- phosphatidyl choline 300 mg, vit B1 6 mg, vit
B12 6 mcg, vit B2 6 mg, vit B6 6 mg, vit E acetate 6 mg

Indications

Acute, subacute & chronic hepatitis; toxic metabolic liver diseases, intoxications (eg
from drugs); infection, fatty degeneration of the liver due to alcohol, hypernutrition,
DM, kwashiorkor, pregnancy; cholestasis; pre- & post-op care, esp in liver/gallbladder
surgery.

Dosage

Essentiale cap Maintenance therapy 1-2 cap tid. Essentiale Forte cap Intensive
therapy 1-2 cap tid for the 1st 2 mth.

Administration

Should be taken with food

Mechanism of Action

Essentiale/Forte regulates membrane permeability and improves the exchange of

substances between the intra- and extracellular space. It activates metabolic function
and supports the energy balance of the liver. It restores enzyme functions and
promotes detoxification of the liver. Neutral fats and cholesterol are transformed into
transportable forms and led to their physiological oxidation. Liver cell regeneration is
stimulated and the bile is stabilized.

MIMS Class

Cholagogues, Cholelitholytics & Hepatic Protectors

ATC Classification

A05BA - Liver therapy ;