Penfluridol, Semap®, Micefal®, Asemap®, Nhwa®

• Semap®
• Micefal®
• Asemap®
• Nhwa®

• 1th generation (Typical) anti-psychotics
• Diphenylbutylpiperidine
• Dopamin Antagonist

• Tablet: 20 mg

• Chronic schizophrenia

Pharmacodynamics:

• Mechanisem of action: blocks the postsynaptic dopamine receptor in the mesolimbic dopaminergic system and inhibits the release of hypothalamic and hypophyseal hormones.

Pharmacokinetics:

 Absorption:

• Orally. Peak plasma concentrations after 2 hours.

Distribution:

 Metabolism:

• Enterohepatic

Excretion:

• Urine and faeces (as N-dealkylated metabolite). Elimination half-life: 36 hours (initial), 120 hours (terminal).

Psychoses (Adult):

• Initial dose: 20-60 mg Po (orally) weekly
• Maximum dose: 250 mg Po (orally) once a week in severe or resistant conditions.

• Orthostatic hypotension with MAOIs
• Increase sedation with alcohol, hypnotics, antihistamines, opiates
• Antacids containing aluminum salts may decrease absorption of Penfluridol
• Additive antimuscarinic effects with TCAs
• Reduce bromocriptine‘s ability to reduce serum prolactin
• Amphetamines may increase psychosis
• Inhibit antiparkinsonian effects of levodopa
• Increase risk of extrapyrimidal symptoms with Metoclopramide
• 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)
• Have additive hypotensive effects with Trazodone
• May increase levels of valproic acid (Enzyme inhibitor effect of Penfluridol).
• Potentially Fatal: May produce neurotoxicity with lithium.
• Food interactions: Avoid valerian, St John’s wort, kava kava, gotu kola => increased risk of CNS depression.

More Frequent:

• Slightly sedative
• Extrapyramidal symptoms: Parkinsonism, rigidity, tremor Akathisia, Tardive Dyskinesiae and pseudo-Parkinsonism.

Less Frequent:

•  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
• Delirium
• Agitation
• Anxiety
• Depression
• Euphoria
• Anorexia
• Constipation
• Diarrhea
• Alopecia
• Amenorrhoea
• Hyperprolactinemia (Leaking milk from breast)
• Hypoglycaemia
• hyponatraemia
• hypersalivation
• Nausea, vomiting
• Bronchospasm
• Venous blood clots, particularly in the legs (the symptoms include swelling, pain and redness in the legs)
• Potentially Fatal side effects: Blood dyscrasias; neuroleptic malignant syndrome; alteration of heart conduction leading to QT prolongation and life threatening arrhythmias.

• MAOIs
• Alcohol, hypnotics, antihistamines, opiates
• Antacids containing aluminum salts
• TCAs
• Hyperprolactinemia due to any cause
• Amphetamines
• Levodopa
• Metoclopramide
• Phenytoin
• Medications cause long Q-T interval: 1a antiarrhythmics, TCAs, some quinolone antibiotics (e.g. Moxifloxacin)
• Trazodone
• valproic acid
• Lithium.
• Valerian, St John’s wort, kava kava, gotu kola

Pregnancy: Category C

Lactation: Not recommended in nursing mother

1. Extremely long elimination half-life and its effects last for many days after single oral dose.

2. Slightly sedative, but often causes extrapyramidal side effects, such as akathisia, dyskinesiae and pseudo-Parkinsonism.

3. Caution in elderlies! do a dose adjustment with close monitoring.

4. Caution in patients with epilepsy!

5. Caution in preexisting cardiac conduction problems; hypokalaemia, hypomagnesemia; hypothyroidism.

6. Use with caution in patients with => liver, heart, kidney diseases

7. Avoid driving and using of machinery while taking Penfuridol => it reduces awareness, sleepiness, dizziness and visual problems associated with the use of this medicine.

8. Caution for Neuroleptic Malignant Syndrome (NMS): hyperpyrexia, muscle rigidity, altered mental status (including catatonic signs), and evidence of autonomic instability (irregular pulse or blood pressure), elevated CPK, myoglobinuria (rhabdomyolysis), and acute renal failure. NMS is potentially fatal, requires intensive symptomatic treatment and immediate discontinuation of neuroleptic treatment.

9. Over-dosage:

• Severe extrapyramidal reactions
• Hypotension (can produce shock like state)
• Sedation
• Treatment: No specific antidote, do a supportive therapy, Heart monitoring, ECG (QT Prolongation), Pulse-Oxymetery, Observe Airway, Breathing, circulation.

10. Caution for Tardive Dyskinesia:

• Rhythmical involuntary movements of the tongue, face, mouth or jaw (e.g. protrusion of tongue, puffing of cheeks, puckering of mouth, chewing movements) Irreversible in some patients in patients treated with neuroleptics with antipsychotic properties and other drugs with substantial neuroleptic activity. The risk of developing tardive dyskinesia may minimize by reducing the dose of the neuroleptic drug used and its duration of administration => anti-Parkinson agents usually do not alleviate the symptoms of this syndrome.

11. Caution in administration of Penfuridol in patients with bone marrow suppression disorders, failures due to any cause => close observation (Complete blood count with differential and absolute neutrophil count in mandatory)

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