Mincof
Mincof Uses, Dosage, Side Effects, Food Interaction and all others data.
Aminophylline is a combination of theophylline and ethylenediamine. Ethylenediamine is inactive; it increases the solubility of theophylline in water. Theophylline relaxes bronchial smooth muscle. Suggested mechanisms are an increase in intracellular cAMP through inhibition of phosphodiesterase; adenosine receptor antagonism, prostaglandin antagonism and effects on intracellular calcium.
Aminophylline is the ethylenediamine salt of theophylline. Theophylline stimulates the CNS, skeletal muscles, and cardiac muscle. It relaxes certain smooth muscles in the bronchi, produces diuresis, and causes an increase in gastric secretion.
Ammonium chloride is an inorganic compound with the formula NH4Cl. It is highly soluble in water producing mildly acidic solutions.
Systemic acidifier. In liver ammonium chloride is converted into urea with the liberation of hydrogen ions ( which lowers the pH) and chloride.
Dimehydrinate was first described in the literature in 1949, and patented in 1950. Early research into dimenhydrinate focused on its role as an antihistamine for urticaria; the treatment of motion sickness was an accidental discovery.
Dimenhydrinate, also known as B-dimethylaminoethyl benzohydrol ether 8-chlorotheophyllinate, is indicated to prevent nausea, vomiting, and dizziness caused by motion sickness. Dimenhydrinate is a combination of Diphenhydramine and 8-chlorotheophylline in a salt form, with 53%-55.5% dried diphenhydramine, and 44%-47% died 8-chlorotheophylline.
The antiemetic properties of dimenhydrinate are primarily thought to be produced by diphenhydramine's antagonism of H1 histamine receptors in the vestibular system while the excitatory effects are thought to be produced by 8-chlorotheophylline's adenosine receptor blockade.
Trade Name | Mincof |
Generic | Aminophylline + Ammonium Chloride + Dimenhydrinate |
Weight | 32mg/5ml, 30mg/5ml, 8mg/5ml |
Type | Syrup |
Therapeutic Class | |
Manufacturer | Pakistan Pharmaceutical Products (pvt) Ltd, |
Available Country | Pakistan |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
It is used for the treatment and prophylaxis of bronchospasm associated with asthma, emphysema and chronic bronchitis. Also used for adults for the treatment of cardiac asthma and left ventricular or congestive cardiac failure.
- Expectorant in cough syrups.
- 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.
Dimenhydrinate is a medication used to prevent and treat nausea, vomiting, vertigo, and motion sickness.
Dimenhydrinate is indicated for the prevention and treatment of nausea, vomiting, or vertigo of motion sickness.
Mincof is also used to associated treatment for these conditions: Acute Exacerbation of Chronic Bronchitis (AECB), Asthma, Bronchial Asthma, Bronchospasm, Chronic Bronchitis, Exacerbation of asthmaAllergic 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, PotassiumDizziness, Labyrinthine disorder, Menière's Disease, Morning Sickness, Motion Sickness, Nausea, Nausea and vomiting, Post Operative Nausea and Vomiting (PONV), Vomiting, Radiation therapy induced nausea and vomiting
How Mincof works
Aminophylline is the ethylenediamine salt of theophylline. After ingestion, theophylline is released from aminophylline, and theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.
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.
Dimenhydrinate is a theoclate salt that separates into diphenhydramine and 8-chlorotheophylline. While the exact mechanism of action is unknown, diphenhydramine is theorized to reduce disturbances to equilibrium through antimuscarinic effects or histamine H1 antagonism. 8-chlorotheophylline may produce excitation through blocking adenosine receptors, reducing the drowsiness produced by diphenhydramine.
Dosage
Mincof dosage
Oral:Chronic bronchospasm:
- Adult: As hydrate: Initially, 225-450 mg bid, increased if necessary.
- Child: >3 yr: As modified-release hydrate: 12 mg/kg daily increased to 24 mg/kg daily in 2 divided doses after 1 wk.
Intravenous:Acute severe bronchospasm:
- Adult: Loading dose: 5 mg/kg (ideal body weight) or 250-500 mg (25 mg/ml) by slow inj or infusion over 20-30 min. Maintenance infusion dose: 0.5 mg/kg/hr. Max rate: 25 mg/min.
- Child: Loading dose: same as adult dose. Maintenance dose: 6 mth-9 yr: 1 mg/kg/hr and 10-16 yr: 0.8 mg/kg/hr.
- Elderly: Dose reduction may be necessary.
- Hepatic impairment: Dose reduction may be necessary.
Tablets should be swallowed whole and not chewed because of the structure of the tablet.
Side Effects
The most common adverse effects are gastric irritation, nausea, vomiting, diarrhea, hematemesis, epigastric pain and tremor. These are usually early signs of toxicity; however, with high doses, ventricular arrhythmias or seizures may be the first signs to appear and reactivation of peptic ulcer, headache, irritability, restlessness, insomnia, twitching, convulsion and reflex hyperexcitability, palpitation, tachycardia, hypotension, circulatory failure, ventricular arrhythmias, and flushing, albuminuria, diuresis and hematuria. Also inappropriate ADH syndrome may occur.
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.
Infants and children experiencing an overdose may lead to hallucinations, convulsions, or death. Adults experiencing an overdose may present with drowsiness, convulsions, coma, or respiratory depression. Treat overdoses with symptomatic and supportive measures including mechanically assisted ventilation.
In mice the oral LD50 is 203 mg/kg, while in rats it is 1320 mg/kg. The intraperitoneal LD50 in mice is 149 mg/kg.
Precaution
Aminophylline should be given with caution to patients with peptic ulceration, hyperthyroidism, hypertension, cardiac arrhythmias or other cardiovascular disease, or epilepsy, as these conditions may be exacerbated. They should also be given withcaution to patients with heart failure, hepatic dysfunction, chronic alcoholism, acute febrile illness, and to neonates and the elderly, since in all of these circumstances theophylline clearance may be decreased, resulting in increases in serum-theophylline concentrations and serum half-life.
Volume of Distribution
- 0.3 to 0.7 L/kg
Data not found.
The volume of distribution of dimenhydrinate is 3-4 L/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 50 mg oral film coated tablet reaches a Cmax of 72.6 ng/mL with a Tmax of 2.7 hours. A 100 mg suppository reaches a Cmax of 112.2 ng/mL with a Tmax of 5.3 hours.
Half Life
7-9 hours
Unknown
The plasma elimination half life of dimenhydrinate is 5-8 hours.
Clearance
- 0.29 mL/kg/min [postnatal age 3-15 days]
- 0.64 mL/kg/min [postnatal age 25-57 days]
- 1.7 mL/kg/min [ 1-4 years]
- 1.6 mL/kg/min [4-12 years]
- 0.9 mL/kg/min [13-15 years]
- 1.4 mL/kg/min [16-17 years]
- 0.65 mL/kg/min [Adults (16-60 years), non-smoking asthmatics]
- 0.41 mL/kg/min [Elderly (>60 years). liver, and renal function]
- 0.33 mL/kg/min [Acute pulmonary edema]
- 0.54 mL/kg/min [COPD->60 years, stable non-smoker >1 year]
- 0.48 mL/kg/min [COPD with cor pulmonale]
- 1.25 mL/kg/min [Cystic fibrosis (14-28 years)]
- 0.31 mL/kg/min [Liver disease -cholestasis]
- 0.35 mL/kg/min [cirrhosis]
- 0.65 mL/kg/min [acute hepatitis]
- 0.47 mL/kg/min [Sepsis with multi-organ failure]
- 0.38 mL/kg/min [hypothyroid]
- 0.8 mL/kg/min [hyperthyroid]
Data not found.
Elimination Route
Excretion: Urine
Dimenhydrinate is predominantly eliminated in the urine. 1-3% of the dissociated diphenhydramine is eliminated in the urine unchanged, while 64% of diphenhydramine is eliminated in the urine as metabolites. The elimination of dimenhydrinate has not been fully studied.
Pregnancy & Breastfeeding use
Use of aminophylline in pregnant women should be balanced against the risk of uncontrolled disease.
Contraindication
Aminophylline should not be administered to patients with hypersensitivity to xanthines or ehylenediamine. It should not be administered to patients with active peptic ulcer, since it may increase the volume and acidity of gastric secretions.
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