Proctil 5mg Tablet 10s

Proctil 5mg Tablet 10s is one of the older phenothiazine derivatives and remains widely used as an antiemetic (treats & prevents nausea & vomiting) and antivertigo agent. It is available as oral tablets, buccal tablets, intramuscular injection, and rectal suppositories.

Compared with metoclopramide (another antiemetic), it has greater central antiemetic efficacy with a similar risk of extrapyramidal effects.

Prochlorperazine works by blocking dopamine D2 receptors in two key brain areas: the chemoreceptor trigger zone (CTZ) of the brainstem, which controls nausea and vomiting, and the mesolimbic and mesocortical pathways, which are involved in psychosis.

Proctil 5mg Tablet 10s is contraindicated in children under 2 years (or those weighing under 9 kgs) due to the risk of severe respiratory depression and dystonic reactions. Long-term high-dose use of Proctil 5mg Tablet 10s may increase the risk of tardive dyskinesia (repetitive, involuntary movements).

Severe nausea and vomiting

Postoperative, chemotherapy-induced, and pregnancy-related (with caution).

Vertigo and labyrinthine disorders

Including Meniere’s disease (vertigo, hearing loss and tinnitus due to a chronic inner ear disorder) and acute peripheral vertigo.

Migraine

Acute attacks, particularly when nausea is prominent.

Psychotic disorders

Schizophrenia, acute mania, and other psychoses (usually at higher doses).

Severe anxiety (short-term, second-line)

When other agents fail to provide relief.

• Effective for severe nausea and vomiting where other antiemetics have failed.

• Particularly useful in vertigo and migraine-associated nausea.

• Available in multiple formulations (oral, buccal, intramuscular, rectal), which is useful for patients who are unable to swallow.

• Rapid onset reaction, especially when administered via IM or rectal routes.

• Buccal form bypasses first-pass metabolism and works quickly.

Common:

• Sedation, drowsiness
• Dry mouth, blurred vision, constipation (anticholinergic effects)
• Postural hypotension (sudden drop in blood pressure upon standing), dizziness
• Restlessness (akathisia)
• Mild extrapyramidal symptoms (EPS) such as tremor, rigidity, and bradykinesia (slow movements)

Uncommon:

• Acute dystonia (especially in young adults and children), which manifests as sustained muscle contraction, abnormal posture, and oculogyric crisis (upward deviation of eyes)
• Galactorrhoea (discharge of milk from breasts), gynaecomastia (enlargement of male breast tissues), menstrual irregularities due to hyperprolactinaemia (abnormally high levels of prolactin)
• Skin photosensitivity
• Weight gain

• Elevated liver enzymes

Serious side effects that require immediate care:

• Neuroleptic malignant syndrome (NMS), which manifests as high fever, severe muscle rigidity, altered consciousness, and autonomic instability
• Tardive dyskinesia (prolonged use), which may present as involuntary movements of the face, tongue, limbs
• Severe acute dystonia, which may cause laryngeal spasm and oculogyric crisis (upward deviation of eyes)
• QT prolongation or arrhythmias (irregular heart rhythm)
• Severe hypotension (especially when the medicine is delivered IM or rectally)
• Agranulocytosis (extremely low white blood cells), aplastic anaemia (rare)
• Severe allergic reactions, hepatotoxicity
• Increased risk of stroke and death in the elderly with dementia-related psychosis

Take Proctil 5mg Tablet 10s exactly as prescribed. For nausea and vomiting in adults, the typical oral dose is taken three to four times daily, while the buccal form is placed between the upper lip and gum twice daily and allowed to dissolve. The IM dose is given every 6–8 hours, while rectal suppositories are used twice daily. Vertigo doses are usually lower. For psychiatric indications, higher doses may be used under specialist supervision. Swallow tablets whole with water. It can be taken with or without food. Avoid alcohol and other CNS depressants while taking Proctil 5mg Tablet 10s. Avoid driving until you know how it affects you. Do not use in children under 2 years or under 9 kg. Avoid sun exposure due to photosensitivity. Report any abnormal movements, muscle stiffness, or fever immediately. Long-term use should be reviewed regularly for tardive dyskinesia.

Prochlorperazine is a phenothiazine derivative that mainly blocks dopamine D2 receptors. It also blocks histamine H1, muscarinic acetylcholine, and alpha-1 adrenergic receptors. Its clinical effects depend on which receptors are blocked and where in the body.

Its antiemetic action comes from D2 blockade in the chemoreceptor trigger zone (CTZ) of the medulla. The CTZ is the part of the brain that detects nausea-causing substances in the blood and triggers vomiting. By blocking D2 receptors here, Proctil 5mg Tablet 10s stops the signals from toxins, drugs, metabolic disturbances, and chemotherapy agents from reaching the vomiting centre. This suppresses nausea and vomiting from a wide range of causes.

In vertigo, prochlorperazine acts on three sites: the CTZ, the vestibular nuclei, and the labyrinthine system (the parts of the brain and inner ear that control balance), through combined dopamine, histamine, and muscarinic blockade. This reduces the spinning sensation and the nausea that often comes with it.

At higher doses used for psychiatric conditions, prochlorperazine blocks D2 receptors in the mesolimbic pathway, reducing the positive symptoms of psychosis such as hallucinations, delusions, and agitation. However, blocking D2 receptors in other pathways causes side effects:

• Blockade in the nigrostriatal pathway causes extrapyramidal side effects such as dystonia (sustained muscle contractions), Parkinsonism (tremor and stiffness), and tardive dyskinesia.

• Blockade in the tuberoinfundibular pathway raises prolactin levels, leading to galactorrhoea, gynaecomastia, and menstrual disturbance.

• Food (NIL): Can be taken with or without food.

• Alcohol (SEVERE): Significantly increases sedation; avoid.

• Caffeine (MILD): May counteract sedation; does not affect efficacy.

• Grapefruit (CAUTION): May increase plasma levels via CYP3A4 inhibition.

Levodopa, dopamine agonists (pramipexole, ropinirole)

SEVERE

Counteracts the action of Proctil 5mg Tablet 10s. Avoid, unless prescribed.

Other antipsychotics, metoclopramide

SEVERE

Additive EPS, NMS, tardive dyskinesia.

QT-prolonging drugs (citalopram, ondansetron, fluoroquinolones, methadone)

SEVERE

Additive QT prolongation; avoid.

CNS depressants (opioids, benzodiazepines, alcohol)

SEVERE

Additive sedation and respiratory depression.

Anticholinergics

MODERATE

Additive anticholinergic effects.

Antihypertensives

MODERATE

Additive hypotension.

Lithium

CAUTION

Risk of severe neurotoxicity (encephalopathy syndrome).

Tramadol, bupropion

CAUTION

Lower seizure threshold.

CYP2D6 inhibitors (fluoxetine, paroxetine)

MODERATE

May raise Proctil 5mg Tablet 10s levels.

• Parkinson’s disease (Contraindicated): Proctil 5mg Tablet 10s can worsen Parkinsonism.

• Severe cardiovascular disease, QT prolongation 9Caution): High risk of arrhythmias.

• Dementia-related psychosis (elderly) (Avoid): High risk of stroke and death.

• Severe respiratory disease, sleep apnoea (Caution): High risk of respiratory depression.

• Epilepsy: Lowers seizure threshold.

• Bone marrow suppression history: Risk of agranulocytosis.

• Severe hepatic impairment: Reduced clearance.

• Closed-angle glaucoma: Anticholinergic effects can precipitate acute attack.

• BPH, urinary retention: Anticholinergic effects can worsen these.

Overdose presents as severe sedation, deep coma, hypotension, extrapyramidal symptoms (dystonia, rigidity), seizures, hypothermia or hyperthermia, cardiac arrhythmias including QT prolongation, and respiratory depression. There is no specific antidote. Management is supportive: airway protection, cardiac and respiratory monitoring, IV fluids and vasopressors (avoid adrenaline due to paradoxical hypotension from unblocked beta effects), and benzodiazepines for seizures. Activated charcoal may help with recent ingestions. Anticholinergics (benztropine, diphenhydramine) are used for acute dystonia. Haemodialysis is ineffective due to high protein binding. Seek immediate emergency care.

Take a missed dose as soon as you remember, unless it is close to the next dose. In such cases, skip the dose. Do not double-dose. For acute nausea or vertigo, a single missed dose is unlikely to cause an issue. For psychiatric use, consistent dosing is more important. Contact your doctor if you have missed several doses.