Eskatrol
Eskatrol - General Information
A phenothiazine antipsychotic used principally in the treatment of nausea; vomiting; and vertigo. It is more likely than chlorpromazine to cause extrapyramidal disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612)
Pharmacology of Eskatrol
Eskatrol is a piperazine phenothiazine related to high-potency neuroleptics such as perphenazine. It shares many of the actions and adverse effects of the antipsychotics.
Eskatrol for patients
Description
--------------------------------------------------------------------------------
This medicine is used to treat psychotic disorders such as hallucinations, delusions and hostility. Phenothiazine drugs may also
be prescribed to prevent and treat nausea and vomiting.
General Information
--------------------------------------------------------------------------------
This information is for educational purposes only. Not every known side effect, adverse effect, or drug interaction is in this
database. If you have questions about your medicines, talk to your healthcare provider.
Proper use of this medicine
--------------------------------------------------------------------------------
Take this medicine exactly as directed. Swallow extended-release capsules whole, do not open. Do not take more of this medicine
than is prescribed by your doctor. If your doctor has given you a suppository, follow these steps: If the suppository feels soft,
hold it under cold, running water for 1 minute. Dip the tip of the suppository in water. Lie down on your left side and raise your
right knee to your chest. (A left-handed person should lie on the right side and raise the left knee.) Using your finger, insert
the suppository into the rectum, about 1/2 to 1 inch in infants and children and 1 inch in adults. Hold it in place for a few moments.
Stand up after about 15 minutes. Wash your hands thoroughly and resume your normal activities.
Missed Dose
--------------------------------------------------------------------------------
Take your next dose as soon as you remember. If it is time for your next dose, skip the missed dose and go back to your regular
schedule. Do not double doses.
Storage
--------------------------------------------------------------------------------
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and
away from excess heat and moisture. Throw away any medication that is outdated or no longer needed.
Possible Side Effects
--------------------------------------------------------------------------------
Contact your health care provider if the following side effects become bothersome or don't go away; dizziness, drowsiness, dry mouth,
rash, constipation, vision changes, difficulty urinating
If you experience involuntary movements, sore throat, pounding heart beat, or unusual bruising or bleeding, notify your doctor at once.
Warnings/Precautions
--------------------------------------------------------------------------------
This medicine may cause drowsiness.
Be cautious when driving or performing other hazardous activities. This medicine can impair judgment.
Overdose
--------------------------------------------------------------------------------
Seek medical attention immediately. For non emergencies, contact your local or regional poison control center
Drug Interactions
--------------------------------------------------------------------------------
Tell your doctor and pharmacist about all other medicines that you are taking, including non-prescription medicines, nutritional
supplements, or herbal products.
Pregnancy/Nursing
--------------------------------------------------------------------------------
This medicine should be taken during pregnancy only when clearly needed. Talk to your doctor about the risks and benefits when using
this medicine during pregnancy. This medicine may be excreted in breast milk. Nursing mothers are advised to talk to their doctors
before breast-feeding.
More Information
--------------------------------------------------------------------------------
For more information about this medicine, talk to your healthcare provider
Eskatrol Interactions
Thiazide diuretics may accentuate the orthostatic hypotension that may occur with phenothiazines.
Antihypertensive effects of guanethidine and related compounds may be counteracted when phenothiazines are used concomitantly.
Concomitant administration of propranolol with phenothiazines results in increased plasma levels of both drugs.
Eskatrol Contraindications
Do not use in comatose states or in the presence of large amounts of central nervous system depressants (alcohol, barbiturates, narcotics, etc.).
- Do not use in pediatric surgery.
- Do not use in children under 2 years of age or under 20 lb.
- Do not use in children for conditions for which dosage has not been established.
Additional information about Eskatrol
Eskatrol Indication: For control of severe nausea and vomiting, also used in management of the manifestations of psychotic disorders.
Mechanism Of Action: Eskatrol blocks the D2 somatodendritic autoreceptor, resulting in the blockade of postsynaptic dopamine receptors in the mesolimbic system and an increased dopamine turnover. The antiemetic effects of prochlorperazine can be attributed to dopamine blockade in the chemoreceptor trigger zone. Eskatrol also blocks anticholinergic and alpha-adrenergic receptors, the blockade of alpha(1)-adrenergic receptors resulting in sedation, muscle relaxation, and hypotension.
Drug Interactions: Amphetamine Decreased anorexic effect, may increase pyschotic symptoms
Benzphetamine Decreased anorexic effect, may increase pyschotic symptoms
Bromocriptine The phenothiazine decreases the effect of bromocriptine
Dextroamphetamine Decreased anorexic effect, may increase pyschotic symptoms
Dexfenfluramine Decreased anorexic effect, may increase pyschotic symptoms
Diethylpropion Decreased anorexic effect, may increase pyschotic symptoms
Fenfluramine Decreased anorexic effect, may increase pyschotic symptoms
Mazindol Decreased anorexic effect, may increase pyschotic symptoms
Methamphetamine Decreased anorexic effect, may increase pyschotic symptoms
Metrizamide Increased risk of convulsions
Guanethidine The agent decreases the effect of guanethidine
Phendimetrazine Decreased anorexic effect, may increase pyschotic symptoms
Phenmetrazine Decreased anorexic effect, may increase pyschotic symptoms
Phentermine Decreased anorexic effect, may increase pyschotic symptoms
Phenylpropanolamine Decreased anorexic effect, may increase pyschotic symptoms
Rivastigmine Possible antagonism of action
Galantamine Possible antagonism of action
Donepezil Possible antagonism of action
Cisapride Increased risk of cardiotoxicity and arrhythmias
Gatifloxacin Increased risk of cardiotoxicity and arrhythmias
Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
Levofloxacin Increased risk of cardiotoxicity and arrhythmias
Sparfloxacin Increased risk of cardiotoxicity and arrhythmias
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Food Interactions: Avoid alcohol.
Take with food.
Take with a full glass of water Avoid excessive quantities of coffee or tea (Caffeine).
Generic Name: Prochlorperazine
Synonyms: Prochloroperazine; Prochlorpromazine; Prochlorperazine maleate; Prochlorperazine edisylate; Prochlorperazin; Prochlorpemazine; Proclorperazine; Procloperazine; Chlorperazine; Chlormeprazine
Drug Category: Antiemetics; Antipsychotics; Phenothiazines
Drug Type: Small Molecule; Approved
Other Brand Names containing Prochlorperazine: Bayer A 173; Buccastem; Compazine; Capazine; Combid; Compro; Emelent; Emetiral; Eskatrol; Kronocin; Meterazin; Meterazin Maleate; Meterazine; Nipodal; Novamin; Pasotomin; Stemetil; Tementil; Temetid; Vertigon;
Absorption: Rapidly absorbed following oral administration
Toxicity (Overdose): Symptoms of central nervous system depression to the point of somnolence or coma. Agitation and restlessness may also occur. Other possible manifestations include convulsions, EKG changes and cardiac arrhythmias, fever and autonomic reactions such as hypotension, dry mouth and ileus; LD50=400mg/kg (orally in mice)
Protein Binding: 91-99%
Biotransformation: Hepatic. Undergoes metabolism in the gastric mucosa and on first pass through the liver, CYP2D6 and/or CYP3A4.
Half Life: 6 to 8 hours
Dosage Forms of Eskatrol: Solution Intravenous
Liquid Intravenous
Tablet Oral
Suppository Rectal
Chemical IUPAC Name: 2-chloro-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine
Chemical Formula: C20H24ClN3S
Prochlorperazine on Wikipedia: https://en.wikipedia.org/wiki/Prochlorperazine
Organisms Affected: Humans and other mammals