Paracetamol, Guaifenesin, Phenylpropanolamine Hydrochloride, Dextromethorphan Hydrobromide, Chlorpheniramine Maleate.
Formulation: Paracetamol 250 mg, Guaifenesin 100 mg, Phenylpropanolamine HCl 25 mg, Dextromethorphan HBr 10 mg, Chlorpheniramine Maleate 1 mg.
Pharmacology: Paracetamol acts mainly in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin synthesis.
Guaifenesin works to loosen sputum and thin bronchial secretions by irritating the gastric mucosa and stimulating secretions of the respiratory tract. This increases the volume of the respiratory fluid and thins mucus.
Phenylpropanolamin acts directly on alpha- and beta-adrenergic receptors in the mucosa of the respiratory tract. Stimulation of alpha-adrenergic receptors produces vasoconstriction, reduces tissue hyperemia, edema, and nasal congestion, and increases nasal airway patency.
Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain by binding to the NMDA glutamatergic receptor.
Chlorpheniramine binds to the histamine (H1) receptor and blocks the action of endogenous histamine - such as pruritic, vasodilation, flushing and bronchoconstriction.
Pharmacokinetics: Paracetamol undergoes glucuronidation (45-55% of the dose) in the liver or in the gut. A small percentage of paracetamol is oxidized by CYP2E1 to form N-acetyl-p-benzo-quinone imine (NAPQI), a toxic metabolite which is then conjugated to glutathione and excreted renally.
Paracetamol (80%) is excreted in the urine after conjugation and about 3% is excreted unchanged.
Guaifenesin is rapidly absorbed from the GI tract. Within seven hours, 60% is rapidly hydrolyzed and then excreted in the urine, with beta-(2-methoxyphenoxy)-lactic acid as its major urinary inactive metabolite.
Phenylpropanolamine has reduced bioavailability of about 38% from gastrointestinal tract because of first pass metabolism by monoamine oxidase in the stomach and liver.
Dextromethorphan is rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier.
Chlorpheniramine is well absorbed in the GI tract and is metabolized in the liver via CYP450 enzymes to active and inactive metabolites which are excreted in the urine.
For the relief of fever, pain and discomfort associated with colds and flu.
Adult: Take 1 capsule every six hours or as prescribed by the physician.
In case the patient forgets to take it, take as soon as they remember and return to their normal dosage cycle. Do not take double dose to make up for missed dose.
This product is not given to patients allergic to any of the ingredients.
Dextromethorphan is contraindicated in patients with asthma as it causes release of histamines.
Patients with the following conditions should be careful in taking Phenylpropanolamine (PPA): High blood pressure, toxic goiter, benign prostatic hypertrophy, heart rate irregularity, glaucoma and if taking antidepressants. Antihistamines may cause drowsiness and dulling of mental alertness where loss of attentions may lead to accidents. This product may be given to pregnant and nursing women if benefit outweighs the risk.
Adverse reactions include drowsiness, abdominal pain, diarrhea, constipation, headache, thickening of bronchial secretions, urinary retention, increased risk of hemorrhagic stroke due to Phenylpropanolamine, CNS depression.
Paracetamol: Alcohol to avoid hepatotoxicity; increase in effects of aceclofenac, aldosterone, atorvastatin, prednisone, NSAIDs and warfarin.
Phenylpropanolamine HCl: Decreased bronchodilatory effects by beta-blockers, clozapine; hypokalemia when taken with diuretics.
Dextromethorphan HBr: Decreased metabolism when taken with celecoxib, chloramphenicol, vitamin D; increased serum levels when taken with colchicine, doxorubicin, and phenytoin; increase the serotonergic activities with sertraline, toloxatone, alosetron, amphetamine and citalopram.
Chlorpheniramine maleate: Alcohol, antihistamines, CNS depressants, and sedatives.
N02BE51 - paracetamol, combinations excl. psycholeptics ; Belongs to the class of anilide preparations. Used to relieve pain and fever.
AC-NEX PH Forte cap
100's