Drug Study
Drug Study
TILLOR
Drug Name Dosages Indications Mechanism of Action Contraindication Special Precautions Adverse Reactions Drug Interactions
(Generic) s
TYPICAL ANTI-PSYCHOTICS
Haloperidol IM: (Schizophrenia): For management of the Haloperidol is a first- Haloperidol is Patient with dementia- Leucopenia, Adrenaline, alcohol,
Initially, 2-10 mg in manifestations of acute generation (typical contraindicated if related psychosis, bipolar extrapyramidal barbiturates, CNS
subsequent doses given and chronic psychotic antipsychotic) which there is disorders, seizures or EEG symptoms, depressants, other
as often as every 60 disorders including exerts its antipsychotic documented abnormalities, risk of falls, hyperkinesia, antipsychotics,
minutes until symptoms schizophrenia, manic action by blocking hypersensitivity to risk of QT prolongation, risk parkinsonism, anticholinergics,
are controlled, states, and drug-induced dopamine D2 receptors in this drug, in factors for stroke, severe CV drowsiness, insomnia, dopaminergic, TCADs,
administer with a psychoses, such as the brain. Parkinson disease, decreased agitation, headache, lithium, antihypertensives,
dosage interval of 4-8 steroid psychosis. disease, dementia gastrointestinal motility, depression, psychotic CYP3A4 inducers
hours. Adjust dose with Lewy body, paralytic ileus, urinary disorder, tardive (e.g. , anticonvulsants,
according to response It may also be useful in comatose patient, retention, BPH, xerostomia, dyskinesia, oculogyric rifampicin, St John's wort),
and tolerability. Max: 18 the management of in any condition visual problems, and narrow crisis, somnolence, drugs that prolong QT
mg daily. aggressive and agitated with the angle glaucoma. dizziness, visual interval
patients, including depressed central disturbances, (e.g. , antiarrhythmics) or
Oral (Schizophrenia, patients with organic nervous system Concomitant use with tachycardia, cause electrolyte imbalance,
mania): adult: 0.5-5 mg mental syndrome or (CNS). Since antidepressants and arrhythmias, ECG diuretics,
2-3 times daily. mental retardation. many drugs anticholinergic agents. changes, weight sympathomimetics,
Maintenance: 3-10 mg (barbiturates, Avoid abrupt withdrawal. changes, GI upset, metoclopramide,
daily. Adjust dose benzodiazepines, Renal and hepatic salivary hypersecretion, phenindione.
according to response and opioids) can impairment, Elderly, anticholinergic effects
and tolerability. cause depression Children and in Pregnancy. (e.g. dry mouth,
to CNS, blurred vision), rash, Altered concentration of
concurrent use of photosensitivity, haloperidol with CYP3A4
haloperidol impaired temperature and CYP2D6 inhibitors and
should be avoided regulation, inducers. May increase
or used with great convulsions, sexual plasma concentration of
caution. dysfunction. tricyclic antidepressant.
Chlorpromazine IM (schizophrenia): 25- Chlorpromazine is a Chlorpromazine is a Hypersensitivity; Parkinson's disease; CV Tardive dyskinesia (on Potentiation of
50 mg repeated every 6-8 typical antipsychotic neuroleptic that acts by preexisting CNS disease; renal or hepatic long-term therapy). anticholinergic effects of
hr. Substitute with oral used for the treatment of: blocking the postsynaptic depression, coma, impairment; cerebrovascular anti-Parkinson agents and
therapy as soon as Schizophrenia (primarily dopamine receptor in the bone-marrow and respiratory disease; Involuntary TCAs may lead to an
possible. the positive symptoms) mesolimbic dopaminergic suppression; jaundice; DM; movements of anticholinergic crisis.
Bipolar I acute manic system and inhibits the phaeochromocyto hypothyroidism; paralytic extremities may also
Oral : 25 mg tid; may be type of manic-depressive release of hypothalamic ma; lactation. ileus; prostatic hyperplasia occur. Additive orthostatic
given as a single 75 mg illness and hypophyseal or urinary retention; Dry mouth, hypotensive effect in
dose at night. Acute agitation marked hormones. epilepsy or history of constipation, urinary combination with MAOIs.
Maintenance: 25-100 mg by explosive seizures; myasthenia gravis; retention, mydriasis,
tid increased to ≥1 g daily hyperexcitable behavior It has antiemetic, pregnancy; elderly agitation, insomnia, Reverses antihypertensive
as required in psychotic out of proportion to the serotonin-blocking, and (especially with dementia), depression and effect of guanethidine,
patients. initial provocation weak antihistaminic and debilitated patients. convulsions; postural methyldopa and clonidine.
To control nausea and properties and slight Avoid direct sunlight. hypotension, ECG
IM (vomiting, vomiting ganglion-blocking changes. Potentially Fatal: Additive
nausea): Initially, 25 mg Persistent singultus activity. depressant effect with
via IM inj, followed by (chronic hiccups) Allergic skin reaction, sedatives, hypnotics,
25-50 mg every 3-4 hr Relief of apprehension amenorrhea, antihistamines, general
until vomiting stops. before surgery gynecomastia, weight anesthetics, opiates and
gain. Hyperglycemia alcohol.
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.
Flupentixol Oral: (depression): Psychoses and Flupentixol is a Hypersensitivity. Patients with convulsive Rigidity, tremors, Potentiates CNS effects of
Initially, 1 mg daily depression thioxanthene Extremely disorders; advanced hepatic, restlessness, tardive alcohol, general anesthetics,
increased after 1 wk to 2 antipsychotic that inhibits excitable and renal, CV or resp disease; dyskinesia, insomnia, hypnotics, anxiolytics and
mg daily and then to a dopamine-mediated overactive tasks requiring mental dryness of mouth, wt opioids. Blocks
max of 3 mg daily, last effects by blocking patients; mania; alertness; elderly (especially gain, sexual antihypertensive effect of
dose should be given not postsynaptic dopamine porphyria; coma; with dementia), and dysfunction, guanethidine
later than 4 p.m. Doses receptors in the CNS. preexisting CNS debilitated patients; galactorrhea and
>2 mg should be given depression; bone- neuroleptics with sedative menstrual disturbances.
in 2 divided doses marrow effect Potentially
supression; Fatal: Neuroleptic
Oral (pyschosis): Initially, phaeochromocyto malignant syndrome
3-9 mg bid, adjusted ma. Lactation. (hyperthermia,
according to response. hypertonicity of
Max: 18 mg daily. skeletal muscles,
unconsciousness and
IM (pyschosis): As autonomic nervous
decanoate: Initially, 20 system instability).
mg (1 ml of a 2% oily
solution) is given as test
dose. After at least 7
days and depending on
the response, subsequent
doses of 20-40 mg may
be given at intervals of
2-4 wk. Usual
maintenance dose: 50
mg every 4 wk to 300
mg every 2 wk. Up to
400 mg wkly may be
used in severe or
resistant cases.
Levopromazine Oral( Schizophrenia): As antipsychotic drug is Levomepromazine is a Comatose state, most common side Reduced effects of
maleate: 25-50/day in 3 commonly used as an phenothiazine with CNS severe CNS All patients should be effect is amphetamines or increased
divided doses, w/ higher antiemetic to alleviate depressant, α-adrenergic- depression, advised that, if they akathisia. Levomepro risk of psychotic symptoms.
dose at night. Non- nausea and vomiting in blocking, antimuscarinic, phaeochromocyto experience fever, sore throat mazine has prominent Reduced effects and
ambulant: 100-200 palliative care settings antihistaminic and ma, blood or any other infection, they sedative and excessive anticholinergic
mg/day. Max: 1g/day. particularly in terminal analgesic activity. It acts by dyscrasia. should inform their anticholinergic/sympat effects with benztropine,
Adjunct in severe illness. blocking dopamine physician immediately and holytic effects (dry trihexyphenidyl, biperiden,
terminal pain; Nausea undergo a complete blood mouth, hypotension,
and vomiting As Sometimes prescribed for receptors in the mesolimbic count. Treatment should be sinus tachycardia, night TCAs, antihistamines,
maleate: 12.5-50 mg 4-8 people who are dopaminergic system. discontinued if any marked sweats) and may cause disopyramide.
hrly. Sedation 10-25 mg terminally ill to help ease changes (hyperleukocytosis, weight gain.
at bedtime. distressing symptoms granulocytopenia) are
such as pain, sickness, observed in the blood count. Sedation or
IV/IM Adjunct in severe restlessness, and somnolence and
terminal pain;Nausea and confusion. Neuroleptic malignant asthenia are frequent,
vomiting syndrome: If unexplained more pronounced at
fever occurs, treatment the start of treatment.
should be discontinued Photosensitivity and
since this may be one of the allergic skin reactions
symptoms of the malignant have occasionally been
syndrome reported with reported.
neuroleptic drugs (pallor,
hyperthermia, autonomic
disorders, consciousness
disorders, muscle rigidity).
Signs of autonomic
dysfunction, such as
sweating and irregular pulse
or blood pressure, may
precede the onset of
hyperthermia and thus
constitute early warning
signs.
ATYPICAL ANTI-PSYCHOTICS
Clozapine Oral (schizophrenia): In Clozapine is an FDA- Clozapine acts an FDA states the Patient with CV or Significant: Orthostatic Enhances the CNS effects of
patients unresponsive approved atypical antagonist to both following Black cerebrovascular disease or hypotension, narcotics, antihistamines and
to, or intolerant to other antipsychotic drug for dopamine and serotonin Box warnings: conditions predisposing to bradycardia, syncope, benzodiazepines. May reduce
antipsychotics: 12.5 mg treatment-resistant receptors. Neutropenia (due hypotension, history of or seizures, decreased therapeutic effect of norepinephri
1-2 times on day 1, schizophrenia. to the risk of risk factors for seizure, risk gastrointestinal
followed by 25 mg 1-2 It binds to the dopamine agranulocytosis) or history of QT motility, urinary Increased plasma level with
times on day 2. D4 with higher affinity Orthostatic prolongation, DM, BPH, retention, BPH CYP1A2 inhibitors (e.g.
than dopamine D2 hypotension urinary retention, xerostomia, visual ciprofloxacin, fluvoxamine, oral
receptor contributing to Seizures xerostomia, decreased problems, CNS contraceptives, caffeine).
Thereafter, may increase the decrease in negative Myocarditis gastrointestinal motility, depression, Decreased plasma level with
dose in increments of symptoms and Dementia (risk of and visual problems. dyslipidemia, CYP1A2 inducers.
25-50 mg daily within extrapyramidal a cardiovascular Smokers. eosinophilia,
14-21 days up to 300 mg symptoms. event) esophageal Increased risk of neuroleptic
daily in divided doses. CYP2D6 poor metabolizers. dysmotility/aspiration, malignant syndrome with lithium
Subsequent increments Patients taking strong extrapyramidal Risk of seizures with valproic acid
of 50-100 mg 1-2 times a CYP2D6 inhibitors. symptoms, risk of fall,
week if required. Usual fever, hyperglycemia, Potentially Fatal: Increased risk o
dose: 200-450 mg daily. Avoid abrupt withdrawal. QT prolongation, myelosuppression with long-actin
Max: 900 mg daily. Renal and hepatic suicidal ideation, depot antipsychotics.
Gradually reduce to a impairment. temperature regulation
suitable maintenance disturbance, deep vein
dose once desired Elderly (not indicated for thrombosis, pulmonary
therapeutic response is use in dementia-related embolism, weight gain,
achieved. psychosis). tachycardia, visual
Pregnancy and lactation. disturbance,
constipation, nausea,
vomiting, dyspepsia,
dizziness, insomnia,
vertigo, and headache.
Risperidone Oral (schizophrenia): Schizophrenia (in adults Risperidone is a Risperidone Patient w/ known CV Weight changes, May enhance effects of
Initially, 2 mg daily, and children aged 13 and Benzisoxazole atypical should not be disease (e.g. history of metabolic changes, and antihypertensives and CNS
may increase to 4 mg on up) antipsychotic w/ mixed given if a known MI or ischemia, heart sedation are a depressants. Increased risk
the 2nd day, adjust Bipolar I acute manic or serotonin dopamine allergy/hypersens failure, conduction significant concern of QT prolongation when
further if needed. Doses mixed episodes as antagonist activity that itivity to abnormalities), with risperidone. given w/ drugs known to
may be given in 1-2 monotherapy (in adults binds to 5-HT2-receptors risperidone or cerebrovascular disease, cause this effect (e.g.
divided doses. and children aged 10 and in the CNS and in the paliperidone (a conditions that would Risperidone may antiarrhythmics, TCAs).
Maintenance: 4-6 mg up) periphery w/ a very high metabolite or predispose to produce
daily. Max: 16 mg daily. Bipolar I acute manic or affinity; binds to risperidone) is hypotension (e.g. extrapyramidal May antagonize the actions
mixed episodes dopamine-D2 receptors present. dehydration, symptoms (EPS) which of levodopa and other
Oral (Manic episode): adjunctive with lithium w/ less affinity. hypovolemia), can include acute dopamine agonists.
Initially, 2 mg once or valproate (in adults) Hallucinogen parkinsonian syndrome, dystonia, akathisia,
daily. May increase in Autism-associated persisting history of seizures or tardive dyskinesia Carbamazepine and other
increments of 1 mg daily irritability (in children perception other conditions that (TD), and parkinsonian enzyme inducers (e.g.
at intervals of at least 24 aged 5 and up. disorder or HPPD may potentially lower features. rifampicin, phenobarbital)
hr. Max: 6 mg daily. may be a relative seizure threshold, pre- may decrease the serum
contraindication existing Serious side effects of levels of the active
IM (schizophrenia): Give for risperidone hyperprolactinemia, and antipsychotic antipsychotic fraction of
oral risperidone for a because some possible prolactin- medications (like risperidone.
few days to assess patients treated dependent tumors. risperidone) can
tolerability prior to with risperidone include neuroleptic Increased plasma
initiating. Patients not for their HPPD Avoid abrupt malignant syndrome concentration w/
stabilised on oral reported that withdrawal. Hepatic or (NMS). Although the fluoxetine, paroxetine or
risperidone: 25 mg every panic and visual renal impairment. pathogenesis of NMS is verapamil.
2 wk. Patients stabilised symptoms not clear, it is a life-
on oral risperidone for intensified. Elderly w/ dementia- threatening condition
at least 2 wk in doses ≤4 related psychosis. that can manifest with
mg daily: 25 mg every 2 Pregnancy and altered mental status,
wk. Patients stabilised lactation. fever, "lead pipe"
on oral risperidone for rigidity, and autonomic
at least 2 wk in doses >4 instability including
mg daily: 37.5 mg every hypertension,
2 wk. Continue oral tachypnea, and
risperidone for the 1st 3 tachycardia.
wk after the 1st inj.
Olanzapine Oral: Olanzapine is a second- An atypical (second- Black box Patient w/ cerebrovascular Causes an increase in Increased olanzapine
generation
Initially, 10 mg daily as a single (atypical)
dose. Adjust generation)
dose according antipsychotic
to response at intervalswarning
of not less than disease or conditions appetite leading to clearance w/ CYP1A2
24 hr w/in the range of 5-20antipsychotic
mg daily. that exerts its action for olanzapine reg predisposing to hyperphagia with a inducers (e.g.
medication. The FDA primarily on dopamine arding dementia- hypotension, history of consequence of weight carbamazepine,
has approved this and serotonin receptors. It related psychosis. blood dyscrasias, bone gain. omeprazole). Inhibits
IM: Initially, 5-10 mg medication for the works on dopamine D2 Elderly patients marrow depression, , metabolism w/ CYP1A2
followed by 5-10 mg as following conditions: receptors in the with dementia myeloproliferative disease, hypertriglyceridemia, inhibitors (e.g.
required 2 hrs later. mesolimbic pathway as who present with history of seizures or hypercholesterolemia fluvoxamine). May
Max: 20 mg/day Schizophrenia if the an antagonist, blocking symptoms of conditions that lower the antagonize effects of
(combined oral and patient is over the age of dopamine from having a psychosis should seizure threshold. IM: levodopa and dopamine
parenteral dose). 13; potential action at the not be Acute MI, unstable angina high potential to cause agonists.
Patients could only Bipolar disorder post-synaptic prescribed olanza bradycardia, recent heart reduced insulin
receive up to 3 injections including mixed or receptor. Olanzapine bind pine due to an surgery. Elderly w/ sensitivity, leading to
in any 24-hr period. manic episodes s loosely to the receptor increased risk of dementia-related psychosis. impaired glucose
and dissociates easily, mortality. Hepatic and renal tolerance.
allowing for normal
dopamine Olanzapine is impairment. Pregnancy and Dyslipidemia, weight
neurotransmission. The contraindicated in lactation. gain, impaired glucose
effect on the D2 patients with a tolerance leading to
receptors leads to a known metabolic syndrome.
decrease in positive hypersensitivity to
symptoms in patients, this medication.
including hallucinations,
delusions, and
disorganized speech,
thought, and
behavior. Olanzapine wor
ks similarly on serotonin
5HT2A receptors in the
frontal cortex as an
antagonist. Its effects on
serotonin lead to a
decrease in negative
symptoms, including
anhedonia, flat affect,
alogia, avolition, and
poor attention.
Quetiapine Oral : As immediate- FDA approved for blocks 5HT1A, 5-HT2, There are As mentioned Quetiapine correlates Increased serum
release/film-coated tab: schizophrenia, acute D1,D2,H1, A1, and A2 currently no before, quetiapine, along with an increased risk concentration with CYP3A4
Initially, 25 mg bid on manic episodes, and receptors. know FDA with other atypical of death in dementia- inhibitors (e.g.
day 1, followed by 50 adjunctive treatment for Quetiapine itself does not contraindications antipsychotics, is associated related psychosis in ketoconazole, ritonavir,
mg bid on day 2, 100 major depressive act on cholinergic or of quetiapine. with an increased risk of elderly patients. nefazodone). Decreased
mg bid on day 3 and 150 disorder; Non-FDA benzodiazepine receptors. However, there death in elderly patients Alongside this risk, serum concentration with
mg bid on day 4. Titrate approved indications However, a metabolite are several with dementia-related neuroleptic malignant CYP3A4 inducers (e.g.
dose according to such as generalized of quetiapine, precautions to be psychosis. syndrome should be a phenytoin, carbamazepine,
response between 300- anxiety disorder. norquetiapine, blocks M1 considered when Precautions are also consideration due to its rifampin).
450 mg daily given in 2 receptors. Blocking of the administering this necessary for patients with a D2 receptor blockage.
divided doses from day D2 receptor in drug. history of cardiac
4 onwards. Max: 750 mesocortical and (PLS REFER TO arrhythmia, hypokalemia, least likely of atypical
mg daily. mesolimbic pathways is PRECAUTIONS and hypomagnesemia. The antipsychotics to cause
indicated in the treatment ) clinician should consider extrapyramidal
Oral (Acute manic): As of schizophrenia for metabolic panels before symptoms. There is an
immediate-release/film- negative and positive starting the drug. In patients increased risk for
coated tab: 50 mg bid for symptoms, respectively. with diabetes mellitus, suicidal thoughts and
day 1, followed by 100 Increased dopamine in patients should have their behavior associated
mg bid for day 2 then 150 these pathways has shown glucose monitored in an with drug treatment in
mg bid on day 3 and 200 to be associated with attempt to avoid major depressive
mg bid on day 4. Adjust schizophrenia. hyperosmolar coma. disorder patients.
in increments up to 200
mg daily according to Somnolence,
response. Usual dose: orthostatic
400-800 mg daily in 2 hypotension, and
divided doses. Max: 800 dizziness are the most
mg daily. As extended- common side effects
release tab: 300 mg once of quetiapine.
daily on day 1, followed
by 600 mg daily on day 2
adjusted according to
response. Usual dose:
400-800 mg once daily.
Oral (MDD): In
combination with other
drugs for major
depression: As extended-
release tab: 50 mg once
daily for days 1 and 2,
dose to be taken at
bedtime, followed by 150
mg once daily for days 3
and 4 then adjusted
according to response.
Usual dose: 150-300 mg
once daily.
Amisulpride Oral: 400-800 mg bid. Acute psychosis. Amisulpride binds Phaeochromocyto Insomnia,
Patient w/ history of epilepsy; Parkinson's anxiety,
disease, CV disease.Reciprocal
Avoid abrupt withdrawal. Renal im
antagonism
Max: 1.2 g daily. selectively to dopamine ma, concomitant Elderly. Pregnancy and lactation. agitation, drowsiness, between levodopa and
Patients w/ D2, D3 receptors in the prolactin- wt gain, acute dystonia, neuroleptics.
predominantly negative limbic system, and has no dependent tumors parkinsonism,
symptoms: 50-300 mg affinity for D1, D4, and (e.g. pituitary akathisia, tardive
daily. D5 receptor subtypes. gland dyskinesia, QT
Low doses prolactinomas or prolongation,
of amisulpride block breast cancer). hypotension,
presynaptic D2, D3 auto Pre-pubertal bradycardia, GI
receptors, thereby children. disorders (e.g.
enhancing dopaminergic Combination w/ constipation, nausea,
transmission levodopa. vomiting, dry mouth),
hyperglycemia; breast
pain, erectile
dysfunction,
amenorrhea,
gynecomastia,
galactorrhea.
Potentially
Fatal: Neuroleptic
malignant syndrome.
Aripiprazole Oral (Schizophrenia): FDA approved and partial agonist at the D2 Aripiprazole is Patient w/ CV disease, the degree of May reduce plasma levels
Initially, 10 mg or 15 mg predominantly used for and 5HT-1A receptors contraindicated in cerebrovascular disease, extrapyramidal w/ CYP3A4 inducers (e.g.
once daily. Maintenance: symptomatic and an antagonist at 5HT- patients with conditions which predispose symptoms (EPS) and carbamazepine). May
15 mg once daily. Adjust management of psychosis 2a. It has a high affinity documented to hypotension metabolic syndromes increase plasma levels w/
dose at intervals of at in patients with for D2, D3, 5HT-1a, and hypersensitivity to or HTN , Parkinson’s are less due to receptor CYP3A4 inhibitors (e.g.
least 2 wk. Max: 30 mg schizophrenia and 5HT2a receptors. it or any disease, suicidal attempts. specificity. clarithromycin,
once daily. monotherapy or component of the Patient at risk of seizures, Aripiprazole is ketoconazole) or CYP2D6
adjunctive therapy for stabilizes dopamine and formula including those w/ history associated with lower inhibitors (e.g. fluoxetine,
Oral (Mania): Initially, acute manic episodes serotonin within the of seizures, head trauma, incidences of weight quinidine).
15 mg once daily, associated with bipolar nucleus accumbens, brain damage. Not intended gain,
increased to 30 mg once disorder. ventral tegmental area, for treatment in elderly w/ hypercholesterolemia,
daily according to and frontal cortex dementia-related psychosis. glucose dysregulation,
response. can also serve as an resulting in the Severe hepatic impairment. cardiovascular
adjunctive treatment for management of positive,
IM (Rapid control of major depressive negative, and cognitive abnormalities, and
agitation and disturbed disorder, and Tourette symptoms in hyperprolactinemia.
behaviour in syndrome schizophrenia
schizophrenia or mania): Other possible side
Initially, 9.75 mg as a effects
single dose by deep inj from aripiprazole inclu
followed by a further de somnolence, nausea,
dose after 2 hr if vomiting, akathisia,
necessary. Dose range: and lightheadedness.
5.25-15 mg as a single
dose. Max: 30 mg daily
(combined oral and
parenteral dose). Patients
could only receive up to 3
inj daily.
REFERENCES:
Basit H, Kahwaji CI. [Updated 2020 May 4]. In: StatPearls. Treasure Island (FL): StatPearls Publishing; 2020 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK556010/
Philippines. (n.d.). Retrieved October 09, 2020, from https://corporate.mims.com/country_office/philippines/