fluPHENAZine decanoate (Rx)
Generic: FluPHENAZine decanoate
Brand: Modecate
(floo-fen'ah-zeen)
Pharmacological Action
Depresses cerebral cortex, hypothalamus, limbic system, which control activity and aggression; blocks neurotransmission produced by dopamine at synapse; exhibits strong a-adrenergic and anticholinergic blocking action; mechanism for antipsychotic effects is unclear
Therapeutic outcome: Decreased signs and symptoms of psychosis
Uses
Schizophrenia
Contraindications
Hypersensitivity, blood dyscrasias, coma, bone marrow depression, closed-angle glaucoma
Precautions: Pregnancy C, breastfeeding, children ,12 yr, geriatric, seizure disorders, hypertension, hepatic/cardiac disease, abrupt discontinuation; accidental exposure, agranulocytosis, ambient temperature increase, angina, hypersensitivity to benzyl alcohol/parabens/sesame oil/tartrazine dye, QT prolongation, suicidal ideation, renal failure, Parkinson's disease, hypocalcemia, head trauma, prostatic hypertrophy, pulmonary disease, infection, ileus, chemotherapy, breast cancer
BLACK BOX WARNING: Increased mortality in elderly patients with dementia-related psychosis
Dosage & Routes
Decanoate Adult and child .12 yr: IM/SUBCUT 12.5-25 mg q1-3 wk, may increase slowly, max 100 mg/dose HCl
Adult: PO 2.5-10 mg, in divided doses q6-8 hr, max 40 mg/day; IM initially 1.25 mg then 2.5-10 mg in divided doses q6-8 hr
Available forms: decanoate: inj 25 mg/ml; elixir 2.5 mg/5 ml; oral sol 5 mg/ml;
HCl: tabs 1, 2.5, 5, 10 mg; inj 2.5 mg/ml
Implementation PO route - Give with food, milk, or a full glass of water to minimize gastric irritation - Oral concentrate: Give using a calibrated measuring device. Dilute just before use with 120-240 ml of water, saline, milk, 7-Up, carbonated orange beverage, or the following juices: apricot, orange, pineapple, prune, tomato or V-8. Do not mix with beverages containing caffeine (coffee, cola), tannics (tea), or pectinates (apple juice) or with other liquid medications. Avoid spilling the solution on the skin and clothing - Oral elixir: Give using a calibrated measuring device. Avoid spilling the solution on the skin and clothing Injectable routes - Visually inspect for particulate matter and discoloration prior to use; slight yellow to amber color does not alter potency, markedly discolored solutions should be discarded IM route (fluPHENAZine HCl only) - No dilution necessary, if irritation occurs, subsequent IM doses may be diluted with NS for injection or 2% procaine - Inject slowly and deeply into the upper, outer quadrant of the gluteal muscle using a dry syringe and needle; aspirate prior to injection - Keep patient in a recumbent position for at least 30 min following injection to minimize hypotensive effects - Rotate the site of injection to avoid irritation or sterile abscess formation with repeat use IM depot injection (fluPHENAZine decanoate or fluPHENAZine enanthate) - FluPHENAZine decanoate or enanthate injections are administered via IM or subcut; do not use IV - FluPHENAZine depot injections must be drawn up using a dry syringe and needle of at least 21-G; do not dilute - Inject slowly and deeply into the upper outer quadrant of the gluteal muscle, aspirate - Keep patient in a recumbent position for at least 30 min following the initial injection to minimize hypotensive effects; once dose-stabilized on depot formulation, this precaution may be modified - Rotate the site of injection to avoid irritation or sterile abscess formation with repeat administration Subcut injection route (fluPHENAZine decanoate or fluPHENAZine enanthate) - FluPHENAZine decanoate or enanthate injections are administered via IM or SC injection only; do not administer intravenously - FluPHENAZine depot injection solutions must be drawn up using a dry syringe and a needle of at least 21-G; do not dilute - Inject subcut taking care not to inject intradermally - Keep patient in a recumbent position for at least 30 min following the initial injection to minimize hypotensive effects. Once dose-stabilized on depot formulation, this precaution may be modified for ambulatory patients; rotate the injection sites
Adverse Effects
CNS: EPS, pseudoparkinsonism, akathisia, dystonia, tardive dyskinesia, drowsiness, headache, seizures, neuroleptic malignant syndrome, drowsiness
CV: Orthostatic hypotension, hypertension, cardiac arrest, ECG changes, tachycardia
EENT: Blurred vision, glaucoma, dry eyes, nasal congestion
GI: Dry mouth, nausea, vomiting, anorexia, constipation, diarrhea, jaundice, weight gain, paralytic ileus, hepatitis, cholecystic jaundice
GU: Urinary retention, urinary frequency, enuresis, impotence, amenorrhea, gynecomastia
HEMA: Anemia, leukopenia, leukocytosis, agranulocytosis, aplastic anemia, thrombocytopenia
INTEG: Rash, photosensitivity, dermatitis, hyperpigmentation (long-term use)
RESP: Laryngospasm, dyspnea, respiratory depression
Pharmacokinetics
Absorption: Well absorbed (PO, IM)
Distribution: Widely absorbed, crosses blood-brain barrier, placenta
Metabolism: Liver, extensively, not dialyzable
Excretion: Kidneys (metabolites)
Half-life: HCl-4.7-15.3 hr, enanthate 3½-4 days, decanoate 6.8-14.3 days
Pharmacodynamics
PO/IM
HCl: Onset 1 hr, Peak 1½-2 hr, Duration 6-8 hr IM
Enanthate: Onset 1-2 days, Peak 2-3 days, Duration 1-3 wk IM
Decanoate: Onset 1-3 days, Peak 1-2 days, Duration .4 wk
Interactions
Individual drugs Alcohol, haloperidol, metyrosine, risperidone: increased effects of both products, oversedation Amiodarone, ARIPiprazole, arsenic trioxide, astemizole, dasatinib, disopyramide, dofetilide, droperidol, erythromycin, flecainide, gatifloxacin, haloperidol, ibutilide, levomethadyl, lurasidone, ondansetron, paliperidone, palonosetron, pimozide, procainamide probucol, ranolazine, quiNIDine, sotalol, sparfloxacin, saquinavir, SUNItinib, vorinostat, ziprasidone: increased QT prolongation, torsades de pointes (at higher doses)
EPINEPHrine: increased toxicity
Levodopa: decreased antiparkinson activity
Lithium: decreased effects of lithium
Drug classifications
Anticholinergics: increased anticholinergic effects
Barbiturates: decreased effect of fluphenazine, oversedation CNS depressants: oversedation
Smoking: decreased effects of fluphenazine
Drug/herb Betel palm, kava: increased EPS Cola tree, hops, kava, nettle, nutmeg: possible increased action Henbane leaf: increased anticholinergic effect
Drug/lab test
Increased: liver function tests, cardiac enzymes, cholesterol, blood glucose, prolactin, bilirubin, cholinesterase
Decreased: hormones (blood and urine) False positive: pregnancy tests, PKU, urinary steroids, 17-OHCS
Nursing Considerations
Assessment - SSRIs, SNRIs, serotonin-receptor agonists: increased serotonin syndrome, malignant neuroleptic syndrome
BLACK BOX WARNING: Increased mortality in elderly patients with dementia-related psychosis; not approved for this use - Serotonin syndrome, neuroleptic malignant syndrome: severe EPS, increased CPK, altered mental state, sinus tachycardia, change in B/P; sweating often occurs in young men; heat stress, physical exhaustion, dehydration, organic brain disease - QT prolongation, torsades de pointes: ECG for changes - Assess mental status: orientation, mood, behavior, presence and type of hallucinations before initial administration and monthly; this product should significantly reduce psychotic behavior - Monitor bilirubin, CBC, liver function tests monthly; ophthalmic exams periodically - Assess affect, orientation, LOC, reflexes, gait, coordination, sleep pattern disturbances - Monitor B/P with patient sitting, standing, and lying down; take pulse and respirations q4 hr during initial treatment; establish baseline before starting treatment; report drops of 30 mm Hg; obtain baseline ECG, Q-wave and T-wave changes - Check for dizziness, faintness, palpitations, tachycardia on rising; severe orthostatic hypotension is common - Assess for EPS including akathisia (inability to sit still, no pattern to movements), tardive dyskinesia (bizarre movements of the jaw, mouth, tongue, extremities), pseudoparkinsonism (rigidity, tremors, pill rolling, shuffling gait); an antiparkinson product should be prescribed - Assess for constipation, urinary retention daily; if these occur, increase bulk, water in diet
Patient/family education - Caution patient to avoid hazardous activities until product response is determined; dizziness, blurred vision may occur - Inform patient that orthostatic hypotension occurs often and to rise from sitting or lying position gradually; tell patient to avoid hot tubs, hot showers, tub baths because hypotension may occur; tell patient that in hot weather, heat stroke may occur; extra precautions are necessary to stay cool - Instruct patient to avoid abrupt withdrawal of this product, or EPS may result; product should be withdrawn slowly - Advise patient that follow-up lab and ophthalmic exams are needed - Teach patient to avoid OTC preparations (cough, hay fever, cold) unless approved by physician because serious product interactions may occur; avoid use with alcohol, CNS depressants; increased drowsiness may occur - Instruct patient to use a sunscreen and sunglasses to prevent burns - Teach patient about EPS and necessity of meticulous oral hygiene because oral candidiasis may occur - Instruct patient to take antacids 2 hr before or after this product - Advise patient to report sore throat, malaise, fever, bleeding, mouth sores; if these occur, CBC should be performed and product discontinued
Evaluation
Positive therapeutic outcome: Decrease in emotional excitement, hallucinations, delusions, paranoia; Reorganization of patterns of thought, speech TREATMENT OF
OVERDOSE: Lavage if orally ingested; provide airway; do not induce vomiting or use EPINEPHrine
Reference
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