Penfluridol

Oral
Psychoses

Preexisting CNS depression or coma.

Pregnancy and lactation; elderly; epilepsy; preexisting cardiac conduction problems; hypokalaemia, hypomagnesemia; hypothyroidism.

Lower threshold for seizures, blurring of vision, dry mouth, retention of urine, constipation, orthostatic hypotension, weight gain, impaired glucose tolerance, allergic skin rashes, cholestatic jaundice; extrapyramidal effects; delirium; agitation, anxiety, depression, euphoria; anorexia, constipation, diarrhoea; alopecia; amenorrhoea, hypoglycaemia; hyponatraemia; hypersalivation, nausea, vomiting; bronchospasm; reported increased risk of breast cancer.
Potentially Fatal: Blood dyscrasias; neuroleptic malignant syndrome; alteration of heart conduction leading to QT prolongation and life threatening arrhythmias.

Symptoms: deep sleep, dystonia, extrapyramidal symptoms. Treatment: supportive and symptom specific.

Orthostatic hypotension with MAOIs; may increase sedation with alcohol, hypnotics, antihistamines, opiates; antacids containing aluminum salts may decrease absorption; additive antimuscarinic effects with TCAs; may reduce bromocriptine's ability to reduce serum prolactin; amphetamines may increase psychosis; may inihibit antiparkinsonian effects of levodopa; may increase risk of extrapyrimidal symptoms with metoclopramide; may increase phenytoin levels (phenytoin may reduce penfluridol levels); possible additive effects on QT interval with type 1a antiarrhythmics, TCAs, some quinolone antibiotics (e.g. moxifloxacin), may have additive hypotensive effects with trazodone; may increase levels of valproic acid.
Potentially Fatal: May produce neurotoxicity with lithium.

Avoid valerian, St John's wort, kava kava, gotu kola; increased risk of CNS depression.

Description: Penfluridol blocks the postsynaptic dopamine receptor in the mesolimbic dopaminergic system and inhibits the release of hypothalamic and hypophyseal hormones.
Duration: 1 wk.
Pharmacokinetics:
Absorption: Absorbed from the GI tract (oral); peak plasma concentrations after 2 hr.
Metabolism: Undergoes enterohepatic recycling.
Excretion: Urine and faeces (as N-dealkylated metabolite). Elimination half-life: 36 hr (initial), 120 hr (terminal).

Antipsychotics