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Drug Study

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CC RUBIE ANN G.

TILLOR

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

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