obat psikiatri umum
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dafter boat psikiatri umumTRANSCRIPT
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,
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,
- 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)