mentex

Uses

1. Expectorant in cough syrups.
2. The ammonium ion (NH4+) in the body plays an important role in the maintenance of acid-base balance. The kidney uses ammonium (NH4+) in place of sodium (Na+) to combine with fixed anions in maintaining acid-base balance, especially as a homeostatic compensatory mechanism in metabolic acidosis. The therapeutic effects of Ammonium Chloride depend upon the ability of the kidney to utilize ammonia in the excretion of an excess of fixed anions and the conversion of ammonia to urea by the liver, thereby liberating hydrogen (H+) and chloride (Cl–) ions into the extracellular fluid. Ammonium Chloride Injection, USP, after dilution in isotonic sodium chloride injection, may be indicated in the treatment of patients with: (1) hypochloremic states and (2) metabolic alkalosis.

Dextromethorphan is used for Chronic dry cough or unproductive cough; Acute dry cough which is interfering with normal function or sleep.

Diphenhydramine is used for the treatment of followings:

• Seasonal, perennial, vasomotor rhinitis
• Urticaria, angioneurotic oedema, anaphylaxis
• Pruiritic conditions
• Premedication for emesis and motion sickness
• Miscellaneous like meniere's disease and parkinsonism

Pseudoephedrine is an alpha and beta adrenergic agonist used to treat nasal and sinus congestion, as well as allergic rhinitis.

Pseudoephedrine is a sympathomimetic amine used for its decongestant activity.

mentex is also used to associated treatment for these conditions: Allergic Reaction, Allergic cough, Common Cold, Cough, Cough caused by Common Cold, Diabetes, High Blood Pressure (Hypertension), Metabolic Alkalosis, Nasal Congestion, Nasal Congestion Due to Allergic Rhinitis, Productive cough, Rhinorrhoea, Sneezing, Bronchial congestion, Dry cough, Excess mucus or phlegm, Hypochloremic state, Airway secretion clearance therapy, Bronchodilation, Parenteral rehydration therapy, Weight Loss, PotassiumAllergic cough, Common Cold, Common Cold/Flu, Cough, Cough caused by Common Cold, Coughing caused by Allergies, Coughing caused by Bronchitis, Coughing caused by Flu caused by Influenza, Fever, Flu caused by Influenza, Headache, Irritative cough, Itching of the nose, Itching of the throat, Nasal Congestion, Pseudobulbar affect, Rhinorrhoea, Sneezing, Upper respiratory symptoms, Watery itchy eyes, Airway secretion clearance therapy, Bronchodilation, Oropharyngeal antisepsisAllergic Rhinitis (AR), Allergic cough, Allergies, Anaphylaxis, Angioedema, Common Cold, Common Cold/Flu, Conjunctival irritation, Cough, Cough Variant Asthma, Cough caused by Common Cold, Eye allergy, Fever, Insect Bites, Insect Stings, Insomnia, Irritative cough, Itching of the nose, Itching of the throat, Motion Sickness, Nasal Congestion, Oral Mucositis, Pain, Parkinsonian Syndromes, Pollen Allergy, Productive cough, Pruritus, Rash, Rhinorrhoea, Sinus Congestion, Sinus headache, Skin Irritation, Sneezing, Sunburn, Symptoms of Acute Bronchitis Accompanied by Coughing, Upper respiratory tract hypersensitivity reaction, site unspecified, Urticaria, Dermatographism, Dry cough, Watery itchy eyes, Airway secretion clearance therapy, ExpectorantAllergic Rhinitis (AR), Allergies, Common Cold, Common Cold Associated With Cough, Common Cold/Flu, Cough, Cough caused by Common Cold, Eye allergy, Fever, Flu caused by Influenza, Headache, Irritative cough, Nasal Allergies, Nasal Congestion, Nasal Congestion caused by Common Cold, Pain, Perennial Allergy, Priapism, Respiratory Allergy, Rhinorrhoea, Seasonal Allergic Rhinitis, Seasonal Allergies, Sinus Congestion, Sinusitis, Sneezing, Sore Throat, Symptoms of Acute Bronchitis Accompanied by Coughing, Throat irritation, Upper Respiratory Tract Infection, Upper respiratory tract congestion, Upper respiratory tract signs and symptoms, Dry cough, Minor aches and pains, Sinus pain, Watery itchy eyes, Airway secretion clearance therapy

How mentex works

Ammonium chloride increases acidity by increasing the amount of hydrogen ion concentrations.

Ammonium chloride can be used as an expectorant due to its irritative action on the bronchial mucosa. This effect causes the production of respiratory tract fluid which in order facilitates the effective cough.

Dextromethorphan is an agonist of NMDA and sigma-1 receptors. It is also an antagonist of α3/β4 nicotinic receptors.[A10589] However, the mechanism by which dextromethorphan's receptor agonism and antagonism translates to a clinical effect is not well understood.

Diphenhydramine predominantly works via the antagonism of H1 (Histamine 1) receptors . Such H1 receptors are located on respiratory smooth muscles, vascular endothelial cells, the gastrointestinal tract (GIT), cardiac tissue, immune cells, the uterus, and the central nervous system (CNS) neurons . When the H1 receptor is stimulated in these tissues it produces a variety of actions including increased vascular permeability, promotion of vasodilation causing flushing, decreased atrioventricular (AV) node conduction time, stimulation of sensory nerves of airways producing coughing, smooth muscle contraction of bronchi and the GIT, and eosinophilic chemotaxis that promotes the allergic immune response .

Ultimately, diphenhydramine functions as an inverse agonist at H1 receptors, and subsequently reverses effects of histamine on capillaries, reducing allergic reaction symptoms . Moreover, since diphenhydramine is a first-generation antihistamine, it readily crosses the blood-brain barrier and inversely agonizes the H1 CNS receptors, resulting in drowsiness, and suppressing the medullary cough center .

Furthermore, H1 receptors are similar to muscarinic receptors . Consequently, diphenhydramine also acts as an antimuscarinic . It does so by behaving as a competitive antagonist of muscarinic acetylcholine receptors, resulting in its use as an antiparkinson medication .

Lastly, diphenhydramine has also demonstrated activity as an intracellular sodium channel blocker, resulting in possible local anesthetic properties .

Pseudoephedrine acts mainly as an agonist of alpha adrenergic receptors and less strongly as an agonist of beta adrenergic receptors.[A10896] This agonism of adrenergic receptors produces vasoconstriction which is used as a decongestant and as a treatment of priapism. Pseudoephedrine is also an inhibitor of norepinephrine, dopamine, and serotonin transporters.

The sympathomimetic effects of pseudoephedrine include an increase in mean arterial pressure, heart rate, and chronotropic response of the right atria. Pseudoephedrine is also a partial agonist of the anococcygeal muscle. Pseudoephedrine also inhibits NF-kappa-B, NFAT, and AP-1.

Dosage

mentex dosage

Adults and Children over 12 years: 15 to 30 mg three to four times per day. However, 60 mg doses up to four times per day have been used without increased side effects.

Children between 6 and 12 years: 5-15 mg up to four times per day.

Children between 2 and 6 years: 2.5-5 mg up to four times per day.

Adult-

• Most allergic conditions: 25-50 mg three times a day with a further 50 mg at night.

Children-

• 1 to 5 years of age: 5 mg i.e., 2.5 ml of elixir 4 times a day
• More than 6 years of age: 10 mg i.e. 5 ml of elixir 4 times a day

Side Effects

Adverse effects with Dextromethorphan are rare, but nausea and dizziness sometimes occur. The drug produces no analgesia or addiction and little or no CNS depression. Excitation, confusion and respiratory depression may occur after overdosage.

Side effect includes sedation, dizziness, tinnitus, fatigue, ataxia, blurred vision, diplopia, euphoria, and epigastric discomfort.

Toxicity

LD50 "Rat" after oral administration is: 1650 mg/kg. Overdosage of Ammonium Chloride has resulted in a serious degree of metabolic acidosis, disorientation, confusion and coma. If metabolic acidosis occur following overdosage, the administration of an alkalinizing solution such as sodium bicarbonate or sodium lactate will serve to correct the acidosis.

Patients administering Ammonium chloride should be watched to the signs of ammonia toxicity including (pallor, sweating, irregular breathing, bradycardia, cardiac arrhythmias, local and general twitching, tonic convulsions and coma). It should be used with caution in patients with high total CO2 and buffer base secondary to primary respiratory acidosis. Intravenous administration should be slow to avoid local irritation and toxic effects.

A dextromethorphan overdose may present as nausea, vomiting, stupor, coma, respiratory depression, seizures, tachycardia, hyperexcitability, toxic psychosis, ataxia, nystagmus, dystonia, blurred vision, changes in muscle reflexes, and serotonin syndrome. Overdose should be managed through symptomatic and supportive measures.

Overdose is expected to result in effects similar to the adverse effects that are ordinarily associated with the use of diphenhydramine, including drowsiness, hyperpyrexia, and anticholinergic effects, among others . Additional symptoms during overdose may include mydriasis, fever, flushing, agitation, tremor, dystonic reactions, hallucinations and ECG changes . Large overdose may cause rhabdomyolysis, convulsions, delirium, toxic psychosis, arrhythmias, coma and cardiovascular collapse . Moreover, with higher doses, and particularly in children, symptoms of CNS excitation including hallucinations and convulsions may appear; with massive doses, coma or cardiovascular collapse may follow .

Although diphenhydramine has been in widespread use for many years without ill consequence, it is known to cross the placenta and has been detected in breast milk . This medication should therefore only be used when the potential benefit of treatment to the mother exceeds any possible hazards to the developing fetus or suckling infant .

Pharmacokinetic studies indicate no major differences in the distribution or elimination of diphenhydramine compared to younger adults . Nevertheless, diphenhydramine should be used with caution in the elderly, who are more likely to experience adverse effects . Avoid use in elderly patients with confusion .

The results of a review on the use of diphenhydramine in renal failure suggest that in moderate to severe renal failure, the dose interval should be extended by a period dependent on Glomerular filtration rate (GFR) .

After intravenous administration of 0.8 mg/kg diphenhydramine, a prolonged half-life was noted in patients with chronic liver disease which correlated with the severity of the disease . However, the mean plasma clearance and apparent volume of distribution were not significantly affected .

LD₅₀=500 mg/kg (orally in rats). Considerable overdosage can lead to myocardial infarction (heart attack), serious ventricular dysrhythmias, coma and death.

The oral LD₅₀ of pseudoephedrine is 2206mg/kg in rats and 726mg/kg in mice.

Patients experiencing an overdose of pseudoephedrine may present with giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty urinating, muscle weakness, muscle tension, anxiety, restlessness, insomnia, toxic psychosis, cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure. Treat overdose with symptomatic and supportive treatment including removal of unabsorbed drug.

Precaution

Do not use Dextromethorphan to control a cough that is associated with smoking, asthma, or emphysema, or a cough that is productive (produces sputum or phlegm).

Caution should be exercised with patients in whom drowsiness is undesirable e.g., drivers, machine operators. Concomitant consumption of alcohol or central nervous system (CNS) depressants will potentiate drowsiness.

Interaction

The following medicines should be taken carefully while concomitantly use with Dextromethorphan: Amiodarone, Fluoexetine, Quinidine, CNS depressants and Monoamine oxidase (MAO) inhibitors.

Diphenhydramine administration significantly reduces the absorption of the antituberculous agent para-aminosalicyclic acid (PAS) from the gastrointestinal tract. CNS depressants may potentiate the sedative action of Diphenhydramine. Anticholinergic drugs may potentiate Diphenhydramine’s anticholinergic side effects.

Volume of Distribution

Data not found.

The volume of distribution of dextromethorphan is 5-6.7L/kg.

Diphenhydramine is widely distributed throughout the body, including the CNS . Following a 50 mg oral dose of diphenhydramine, the volume of distribution is in the range of 3.3 - 6.8 l/kg .

The apparent volume of distribution of pseudoephedrin is 2.6-3.3L/kg.

Elimination Route

Completely absorbed within 3–6 h. In healthy persons, absorption of ammonium chloride given by mouth was practically complete. Only 1 to 3% of the dose was recovered in the feces.

A 30mg oral dose of dextromethorphan reaches a C_max of 2.9 ng/mL, with a T_max of 2.86 h, and an AUC of 17.8 ng*h/mL.

Diphenhydramine is quickly absorbed after oral administration with maximum activity occurring in approximately one hour . The oral bioavailability of diphenhydramine has been documented in the range of 40% to 60%, and peak plasma concentration occurs about 2 to 3 hours after administration .

A 240mg oral dose of pseudoephedrine reaches a C_max of 246.3±10.5ng/mL fed and 272.5±13.4ng/mL fasted, with a T_max of 6.60±1.38h fed and 11.87±0.72h fasted, with an AUC of 6862.0±334.1ng*h/mL fed and 7535.1±333.0ng*h/mL fasted.

Half Life

Unknown

Dextromethorphan has a half life of 3-30 hours.

The elimination half-life ranges from 2.4-9.3 hours in healthy adults . The terminal elimination half-life is prolonged in liver cirrhosis .

The mean elimination half life of pseudoephedrine is 6.0h.

Clearance

Data not found.

Values for plasma clearance of a 50 mg oral dose of diphenhydramine has been documented as lying in the range of 600-1300 ml/min .

A 60mg oral dose of pseudoephedrine has a clearance of 5.9±1.7mL/min/kg.

Elimination Route

Excretion: Urine

The metabolites of diphenhydramine are conjugated with glycine and glutamine and excreted in urine . Only about 1% of a single dose is excreted unchanged in urine . The medication is ultimately eliminated by the kidneys slowly, mainly as inactive metabolites .

55-75% of an oral dose is detected in the urine as unchanged pseudoephedrine.

Pregnancy & Breastfeeding use

Pregnancy: Adequate and well-controlled studies in human have not been done. However, Dextromethorphan has not been reported to cause birth defects.

Lactation: It is not known whether dextromethorphan passes into breast milk. However, Dextromethorphan has not been reported to cause problems in nursing babies.

Category B: There are no adequate and well controlled studies in pregnant women using diphenhydramine hydrochloride. Therefore, diphenhydramine hydrochloride should be used in pregnancy only if clearly needed. Diphenhydramine hydrochloride has been reported to be excreted in breast milk and thus, use of diphenhydramine hydrochloride in lactating mother is not recommended.

Contraindication

Hypersensitivity to Dextromethorphan or any other component.

Known hypersensitivity to Diphenhydramine Hydrochloride, Ammonium chloride is contra-indicated in presence of impaired hepatic or renal function.

Acute Overdose

Symptoms: In mild overdose, tachycardia, hypertension, vomiting, mydriasis, diaphoresis, nystagmus, euphoria, loss of motor coordination, and giggling; in moderate intoxication, in addition to those listed above, hallucinations and a plodding ataxic gait; in severely intoxication, agitation or somnolence.

Management: treatment is symptomatic and supportive. Naloxone may be useful in reversing toxicity.

Symptoms: Impaired consciousness; psychosis, seizures, antimuscarinic symptoms (e.g. mydriasis, tachycardia, tachyarrhythmias), resp failure, rhabdomyolysis; acute delirium with visual and auditory hallucination (topical).

Management: Supportive and symptomatic treatment. Convulsions and marked CNS stimulation may be treated with IV diazepam.

Storage Condition

Store at 15-30° C

Store between 15-30° C. Protect from moisture.

Innovators Monograph

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