obat psikiatri umum

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DRUG PREPARATION MOA DOSAGE ADVERSE EFFECT COUNTERACT Benzodiazepine Alprazolam Alprazolam - tab 0.25/0.5/1 mg Xanax, Xanax XR - tab 0.25/0.5/1 mg - tab XR 0.5/1 mg Atarax - tab 0.5 mg Alviz - tab 0.5/1 mg - anxiety, panic dis. - anxiolytic, hypnotic, amnesic, muscle relaxant, anticonvulsant - bind nonspecifically to benzodiazepine receptors BNZ1 (mediates sleep) & BNZ2 (affects muscle relaxation, anticonvulsant activity, motor coordination, memory) > enhance effect of GABA by increasing GABA affinity for GABA receptor Adult Anxiety - initial: 0.25-0.5 mg PO tdd - max: 4 mg/d PO Panic Dis. - initial: 0.5 mg PO tdd - usual: 1-10 mg/d PO Depression - initial: 0.5 mg PO tdd - usual: 3 mg/d PO - max: 4.5 mg/d PO Geriatric - initial: 0.25 mg PO bdd-tdd drowsiness, disinhibition, jaundice (very rare), hallucinations (rare), dry mouth (infrequent), ataxia-slurred speech, suicidal ideation (rare), urinary retention (infrequent), skin rash- respiratory depression-constipation, anterograde amnesia-concentration problems, dizziness-lightheadedness- fatigue-unsteadiness-impaired coordination-vertigo, aggression, rage, hostility, twitches, tremor, mania, agitation, hyperactivity, restlessness Clobazam Clobazam - tab 10 mg Frisium, Clofritis - tab 10 mg - anxiety (w/-w/o depression), insomnia - bind at distinct binding sites associated with chloride ionopore at post-synaptic GABA receptor > increase duration chloride ionopore is open > hyper polarization & stabilization of membrane occur as post-synaptic inhibitory effect GABA enhanced Anxiety - usual: 20-30 mg/d PO - max: 60 mg/d PO ataxia, somnolence, diplopia, dysarthria, Gelastic seizures, Stevens-Johnson syndrome, Toxic Epidermal Necrolysis, urticaria, rash Lorazepam Lorazepam - tab 0.5/1/2 mg Ativan - tab 0.5/1 mg Merlopam - tab 0.5/2 mg - anxiety (w/-w/o depression), insomnia - bind to allosteric site on GABA-A receptors (pentameric ionotropic receptors) > potentiate effect of inhibitory neurotransmitter GABA > open chloride channel in receptor > allow chloride influx > cause hyperpolarization of neuron Anxiety - initial: 1 mg PO bdd- tdd - usual: 1-2 mg PO bdd- tdd - max: 10 mg/d PO Insomnia - 2-4 mg PO bedtime sedation, blood pressure, confusion, ataxia, dizziness, weakness, unsteadiness, cognitive impairment, behavioural disinhibition, respiratory depression, amnesic effect Tricyclic Antidepressant Amitryptilli ne Amitryptilline - tab 25mg - depression - metabolized to nortriptyline > inhibit reuptake of norepinephrine-serotonin almost equally > inhibit membrane pump mechanism responsible for uptake of norepinephrine-serotonin in Depression Adult - initial: 25-100 mg PO tdd-qdd or 50-100 mg PO bedtime - usual: 25-150 mg/d PO Geriatric dizziness, headache, weight gain, cognitive effects (delirium, confusion), mood disturbances (anxiety, agitation), cardiovascular (orthostatic hypotension, sinus tachycardia), sexual ( libido, impotence), sleep disturbance (drowsiness, insomnia)

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Page 1: Obat Psikiatri Umum

DRUG PREPARATION MOA DOSAGE ADVERSE EFFECT COUNTERACTBenzodiazepineAlprazolam Alprazolam

- tab 0.25/0.5/1 mgXanax, Xanax XR- tab 0.25/0.5/1 mg- tab XR 0.5/1 mgAtarax- tab 0.5 mgAlviz- tab 0.5/1 mg

- anxiety, panic dis.- anxiolytic, hypnotic, amnesic, muscle relaxant, anticonvulsant- bind nonspecifically to benzodiazepine receptors BNZ1 (mediates sleep) & BNZ2 (affects muscle relaxation, anticonvulsant activity, motor coordination, memory) > enhance effect of GABA by increasing GABA affinity for GABA receptor

AdultAnxiety- initial: 0.25-0.5 mg PO tdd- max: 4 mg/d POPanic Dis.- initial: 0.5 mg PO tdd- usual: 1-10 mg/d PODepression- initial: 0.5 mg PO tdd- usual: 3 mg/d PO- max: 4.5 mg/d POGeriatric- initial: 0.25 mg PO bdd-tdd

drowsiness, disinhibition, jaundice (very rare), hallucinations (rare), dry mouth (infrequent), ataxia-slurred speech, suicidal ideation (rare), urinary retention (infrequent), skin rash-respiratory depression-constipation, anterograde amnesia-concentration problems, dizziness-lightheadedness-fatigue-unsteadiness-impaired coordination-vertigo, aggression, rage, hostility, twitches, tremor, mania, agitation, hyperactivity, restlessness

Clobazam Clobazam- tab 10 mgFrisium, Clofritis- tab 10 mg

- anxiety (w/-w/o depression), insomnia- bind at distinct binding sites associated with chloride ionopore at post-synaptic GABA receptor > increase duration chloride ionopore is open > hyper polarization & stabilization of membrane occur as post-synaptic inhibitory effect GABA enhanced

Anxiety- usual: 20-30 mg/d PO- max: 60 mg/d PO

ataxia, somnolence, diplopia, dysarthria, Gelastic seizures, Stevens-Johnson syndrome, Toxic Epidermal Necrolysis, urticaria, rash

Lorazepam Lorazepam- tab 0.5/1/2 mgAtivan- tab 0.5/1 mgMerlopam- tab 0.5/2 mg

- anxiety (w/-w/o depression), insomnia- bind to allosteric site on GABA-A receptors (pentameric ionotropic receptors) > potentiate effect of inhibitory neurotransmitter GABA > open chloride channel in receptor > allow chloride influx > cause hyperpolarization of neuron

Anxiety- initial: 1 mg PO bdd-tdd- usual: 1-2 mg PO bdd-tdd- max: 10 mg/d POInsomnia- 2-4 mg PO bedtime

sedation, blood pressure, confusion, ataxia, dizziness, weakness, unsteadiness, cognitive impairment, behavioural disinhibition, respiratory depression, amnesic effect

Tricyclic AntidepressantAmitryptilline Amitryptilline

- tab 25mg- depression- metabolized to nortriptyline > inhibit reuptake of norepinephrine-serotonin almost equally > inhibit membrane pump mechanism responsible for uptake of norepinephrine-serotonin in adrenergic and serotonergic neurons > potentiate or prolong neuronal activity (reuptake = terminate transmitting activity)

DepressionAdult- initial: 25-100 mg PO tdd-qdd or 50-100 mg PO bedtime- usual: 25-150 mg/d POGeriatric- initial: 10 mg PO tdd or 20 mg PO bedtimePTSD/Somatoform- initial: 75 mg/d PO- usual: 150-300 mg/d PO

dizziness, headache, weight gain, cognitive effects (delirium, confusion), mood disturbances (anxiety, agitation), cardiovascular (orthostatic hypotension, sinus tachycardia), sexual ( libido, impotence), sleep disturbance (drowsiness, insomnia)

Tetracyclic AntidepressantMaprotilline Maprotiline HCl

- tab 10/25/50 mgLudiomil- tab 10/25 mgSandepril- tab 50 mg

- depression, anxiety- sedative- inhibit presynaptic uptake of catecholamines > increase concentration at synaptic clefts of brain > act as antagonist at central presynaptic α2-adrenergic inhibitory autoreceptors & hetero-receptors > result in increase in central

Adult- initial: 75 to 100-150 mg/d PO- usual: 75-150 mg/d POGeriatric- initial: 25 mg/d PO- usual: 50-75 mg/d PO

dizziness, drowsiness, somnolence-fatigue, dry mouth, constipation, vertigo, nausea (rare)-vomiting, appetite-weight gain, orthostatic hypotension-hypertension-sinus tachycardia-heart block-arrhythmias, sexual dysfunction (men: impotence, priapism, delayed ejaculation, anejaculation, libido; women: libido, vaginal dryness, painful sexual intercourse, anorgasmia), allergic skin reactions,

Page 2: Obat Psikiatri Umum

noradrenergic & serotonergic activity > moderate peripheral α1 adrenergic antagonist > inhibit amine transporter, delay reuptake of noradrenaline-norepinephrine > strong inhibitor of histamine H1 receptor

photosensitivity, agitation-confusion, induction hypomania or mania, psychotic symptoms, tremor, extrapyramidal symptoms, headache, seizures (at high doses), leukopenia-agranulocytosis (rare), fever, urinary retention

Selective Serotonin Reuptake Inhibitor (SSRI)Fluoxetin Fluoxetin

- caps 10/20 mgAntiprestin- caps 10/20 mgElizac, Zac- caps 20 mg

- depression, obsessive-compulsive dis.- metabolized to norfluoxetine > block reuptake serotonin at serotonin reuptake pump of neuronal membrane > enhance action of serotonin on 5HT1A autoreceptors

Depression/OCD- initial: 20 mg PO sdd- usual: 20-60 mg/d PO- max: 80 mg/d POPanic Dis.- initial: 10 mg PO sdd- usual: 20-60 mg/d PO- max: 60 mg/d PO

abnormal dreams, abnormal ejaculation, anorexia, anxiety, asthenia, diarrhea, dry mouth, dyspepsia, flu syndrome, impotence, insomnia, libido, nausea, nervousness, pharyngitis, rash, sinusitis, somnolence, sweating, tremor, vasodilatation, yawning, agitation, urticaria (hives), itchiness

Sertraline Sertraline- tab 50 mgZoloft, Zerlin, Fridep- tab 50 mg

- depression, anxiety- selective inhibit reuptake of serotonin at presynaptic membrane > increase synaptic concentration serotonin in CNS > enhance serotonergic neurotransmission

Depression/OCD- initial: 50 mg PO sdd- max: 200 mg PO sddPanic Dis./PTSD/Social Anxiety- initial: 25 mg PO sdd- usual: 50 mg PO sdd- max: 200 mg PO sdd

fatigue, insomnia, somnolence, nausea, dry mouth, diarrhea, headache, ejaculation disorder, dizziness, agitation, anorexia, constipation, dyspepsia (indigestion), libido, sweating, tremor, vomiting, impaired concentration, nervousness, palpitations, sweating, hot flushes, / weight, myoclonus, hypertonia, bruxism (teeth grinding), hypoaesthesia, menstrual irregularities, sexual dysfunction, rash, vision abnormal, asthenia, chest pain, paraesthesia. tinnitus

Serotonin-Norepinephrine Reuptake InhibitorVenlafaxine Venlafaxine HCl

- tab 75 mgEfexor XR- tab 75 mg

- depression, generalized anxiety dis., panic dis., social anxiety dis.- inhibit reuptake of serotonin-norepinephrine with potency greater for 5-HT than NE reuptake process > weak inhibitory effects on reuptake dopamine > not active: histaminergic, muscarinic, alpha(1)-adrenergic receptors

Depression- initial: 75 mg PO sdd- max: 225-375 mg/d POAnxiety- initial: 75 mg PO sdd- max: 225 mg/d POPanic Dis.- initial: 37.5 mg PO sdd- max: 225 mg/d PO

headache, nausea, insomnia, asthenia, dizziness, ejaculation/orgasm disorder, somnolence, dry mouth, sweating, constipation, nervousness, abnormal vision, hypertension, impotence, paresthesia, tremor, vasodilation, vomiting, weight loss, chills, palpitations, confusion, depersonalization, night sweats, menstrual disorder (e.g. menorrhagia, metrorrhagia), urinary frequency, abnormal dreams, libido, muscle tonus, sweating, urinary hesitancy, serum cholesterol

Phenothiazine (Typical Antipsychotic)Haloperidol Haloperidol

- tab 0.5/1.5/2/5 mg- drops 2 mg/ml- inj 5/50 mg/mlSerenace- tab 1.5/5 mgLodomer- tab 2/5 mg- drops 2 mg/ml- inj 5 mg/mlHaldol Decanoas- inj 50 mg/ml

- schizophrenia, agitation, behavior problem- depress CNS at subcortical level of brain, midbrain, and brain stem reticular formation > inhibit ascending reticular activating system of brain stem (possibly through caudate nucleus) > interrupt impulse between diencephalon and cortex > antagonize actions of glutamic acid within extrapyramidal system and inhibitions of catecholamine receptors > strong central antidopaminergic and weak central anticholinergic activity

PsychosisAdult- initial: 0.5-5 mg PO bdd-tdd- usual: 1-30 mg/d POGeriatric- initial: 0.5-2 mg PO bdd-tdd- usual: 1-30 mg/d POMania- initial: 0.5-5 mg PO bdd-tdd- usual: 1-30 mg/d PO

extrapyramidal (dystonia, muscle rigidity, akathisia, Parkinsonism), hypotension, anticholinergic (constipation, dry mouth, blurred vision), somnolence

Chlorpromazine

Chlorpromazine- tab 25/100 mg

- schizophrenia, psychosis, anxiety- antagonist dopaminergic-receptors

Psychosis- initial: 10-25 mg PO tdd

sedation, somnolence, extrapyramidal, weight gain, orthostatic hypotension, dry mouth,

Page 3: Obat Psikiatri Umum

- inj 50 mg/ 2mlCepezet- tab 100 mg- inj 50 mg/ 2ml

(D1, D2, D3, D4), serotonergic-receptors (5-HT1, 5-HT2), histaminergic-receptors (H1), alpha1/alpha2-receptors (antisympathomimetic), muscarinic (cholinergic) (M1/M2)

- usual: 200 mg/d POMania- initial: 10 mg tdd-qdd to 25 mg bdd-tdd PO- usual: 25-50 mg PO tdd

constipation, ECG change, contact dermatitis, photosensitivity, urticaria (hives), maculopapular, petechial/ edematous reaction, hyperprolactinaemia, impaired thermoregulation, hyperglycaemia, hhypothalamic abnormalities, blurred vision, mental confusion, ANA titre, SLE cells (+), mydriasis, atonic colon, seizure, agitation, excitement, restlessness

Atypical AntipsychoticRisperidone Risperidone

- tab 1/2/3 mgNeripros- tab 1/2/3 mg- oral sol 1 mg/mlPersidal- tab 1/2/3 mgRisperdal- oral sol 1 mg/ml

- schizophrenia, bipolar dis.- blockade of dopaminergic D2 receptors in limbic system, serotonergic 5-HT2 receptors in mesocortical tract, dopamine receptors in nigrostriatal pathway not affected (extrapyramidal avoided)

Schizophrenia- initial: 2 mg/d PO- titration: 1-2 mg/d PO- target: 4-8 mg/d PO- max: 16 mg/d POBipolar- initial: 2-3 mg/d PO- titration: 1 mg/d PO- target: 1-6 mg/d PO- max: 6 mg/d PO

rash, hyperprolactinaemia, weight gain, seborrhea, constipation, diarrhea, salivation, appetite, indigestion, nausea, vomiting, upper abdominal pain, xerostomia, akathisia, dizziness, dyspnea, asthenia, agitation, urinary incontinence, arthralgia, myalgia, epistaxis, somnolence, sleep disturbances, dose-dependent extrapyramidal (dystonia, tremor, Parkinsonism), blurred vision, anxiety, cough, nasal congestion, nasopharyngitis, fatigue, general pain, gynecomastia, galactorrhea

Mood StabilizerValproic Acid Divalproat Na

- tab 250 mg- tab ER 250/500 mgDepakote- tab 250 mg- tab ER 250/500 mgIkalep- tab 300 mg

- anticonvulsant, seizure, mood dis.- dissociates to valproate ion in GI tract > bind to & inhibit GABA transaminase > inhibit enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings > increase brain concentrations of gamma-aminobutyric acid (GABA) > suppress repetitive neuronal firing through inhibition of voltage-sensitive sodium channels

Mania- initial: 750 mg/d PO- max: 60 mg/kg/d PO

nausea, vomiting, diarrhea, headache. platelet count-tremor (dose-related), hair loss (temporary), drowsiness, dizziness, female hyperandrogenism, double vision, indigestion, lazy eye, infection, tinnitus, aminotransferase concentrations (dose-related), paresthesia, abdominal pain, appetite, weight gain, ataxia, polycystic ovaries, memory impairment, menstrual irregularities, rash, back pain, mood change, anxiety, confusion, abnormal gait, hallucinations, catatonia, dysarthria, tardive dyskinesia, vertigo, blood ammonia

AntimuscarinicTrihexyphenidil

Trihexyphenidil- tab film-coated 2 mg

- antiparkinsonian- selective M1 muscarinic acetylcholine receptor antagonist > discriminate between M1 (cortical or neuronal) & peripheral muscarinic subtypes (cardiac and glandular) > partially blocks cholinergic activity in CNS > increase availability of dopamine

Extrapyramidal- initial: 1 mg/d PO- usual: 5-15 mg/d POParkinson- initial: 1 mg/d PO- usual: 6-10 mg/d PO

drowsiness, vertigo, headache, dizziness, nervousness, agitation, anxiety, delirium, confusion, blurred vision, dry mouth, impaired sweating, abdominal discomfort, constipation, tachycardia, allergic skin reactions, orthostatic hypotension, mydriasis (w/-w/o photophobia)