Rhinathiol Promethazine

Rhinathiol Promethazine

carbocisteine + promethazine

Manufacturer:

sanofi-aventis

Distributor:

DKSH
Full Prescribing Info
Contents
Carbocisteine, promethazine hydrochloride.
Description
(See table.)

Click on icon to see table/diagram/image

*Qualitative composition of the cocoa flavoring: tincture of vanilla, tincture of cocoa with vanillin, acid esters: acetic; butyric; caproic; isobutyric; valeric, alcohol esters: ethylic; butylic; amylic; hexylic, and solvent: ethylic alcohol; propylene glycol.
Alcohol content of the syrup: 3.09% (v/v).
One 5 ml measuring spoon contains 100 mg of carbocisteine, 2.5 mg of promethazine hydrochloride, 3 g of sucrose and 122 mg of anhydrous ethanol.
One 15 ml tablespoon contains 300 mg of carbocisteine, 7.5 mg of promethazine hydrochloride, 9 g of sucrose and 366 mg of anhydrous ethanol.
Action
Pharmacotherapeutic code: ANTIHISTAMINE FOR SYSTEMIC USE. ATC code: R06AD02. (R: Respiratory system).
Pharmacology: Pharmacodynamics:
Promethazine: Promethazine, of the phenothiazine class with aliphatic side chain, is an antihistaminic neuroleptic which is characterized by: a marked sedative effect at the usual doses, of histaminergic origin and central adrenergic blocking; an anticholinergic effect, responsible for peripheral adverse effects; a peripheral adrenergic blocking effect, with possible hemodynamic consequences (risk of postural hypotension); an anti-dopaminergic effect.
Antihistamines share the property of blocking the effects of histamine, particularly on the skin, bronchi, vessels, intestine and conjunctival and nasal mucous membranes, by more or less reversible competitive antagonism.
In most cases, they have a cough suppressant effect which in itself is moderate, but potentiates the effects of centrally-acting morphine cough suppressants, as well as those of other bronchodilators such as sympathomimetic amines with which they are often co-administered.
Pharmacokinetics: Carbocisteine: Orally administered carbocisteine is rapidly absorbed. Peak plasma concentrations are reached in two hours.
Bioavailability is low (less than 10% of the administered dose), probably as a result of intraluminal metabolism and a marked liver first-pass effect.
Elimination half-life is approximately two hours.
Carbocisteine and its metabolites are eliminated primarily in the kidneys.
Promethazine: The bioavailability of promethazine is between 13 and 40%.
Peak plasma concentrations are reached within 1.5 to 3 hours.
The volume of distribution is high due to the liposolubility of the compound, approximately 15 L/kg.
The drug is 75-80% plasma protein bound.
The half-life is between 10 and 15 hours.
Metabolism consists of sulfoxidation followed by demethylation.
Renal clearance represents less than 1% of total clearance and approximately 1% of administered promethazine is detected unchanged in the urine.
The metabolites found in the urine, particularly in sulfoxide form, represents approximately 20% of the dose.
Kidney/liver failure: risk of accumulation of antihistamines in patients with kidney or liver failure.
Indications/Uses
Symptomatic treatment of troublesome, non-productive cough, particularly occurring at night.
Dosage/Direction for Use
FOR ADULTS AND CHILDREN OVER THE AGE OF 2 YEAR ONLY.
Symptomatic treatment should be for a short period (a few days) and restricted when cough occurs.
Adults: 3 to 4 tablespoons (1 tablespoon = 15ml) per day, in divided doses.
Children: use the measuring spoon supplied with this syrup: 25 to 30 months: 3 to 4 of the 5ml measuring-spoonfuls per day, in divided doses.
30 months to 12 years: 4 to 6 of the 5ml measuring-spoonfuls per day, in divided doses.
12 to 15 years: 6 to 9 of the 5ml measuring spoonfuls per day, in divided doses.
This medicine should preferably be taken in the evening, because of the marked sedative effect of promethazine.
Overdosage
Signs of promethazine overdose: seizures (especially in children); consciousness disorders, coma.
Symptomatic treatment is to be instituted in a specialized environment.
Contraindications
Hypersensitivity to the active substances or to any of the excipients (particularly methyl parahydroxybenzoate and other parahydroxybenzoate salts).
Due to the presence of promethazine: Infants (under two years of age) (see Precautions);
History of agranulocytosis;
Risk of urinary retention related to urethro-prostatic disorders;
Risk of angle-closure glaucoma;
Breastfeeding (see Use in Pregnancy & Lactation).
This medicinal product should NOT BE USED: during pregnancy (see Use in Pregnancy & Lactation).
Warnings
CAUTION: THIS MEDICINAL PRODUCT CONTAINS ALCOHOL.
The alcohol content of the syrup is 3.09%, i.e. 122 mg of alcohol per measuring spoonful (5 ml), 366 mg of alcohol per tablespoonful (15 ml).
Special Precautions
This product contains promethazine hydrochloride. It should not be used in pediatric patients less than 2 years of age because of the potential for fatal respiratory depression.
To be used with caution and on doctor's/pharmacist's advice in children 2 to 6 years of age.
Productive coughs, which is a fundamental bronchopulmonary defense mechanism, should be taken seriously.
It is irrational to combine an expectorant or a mucolytic agent with this cough suppressant.
Before prescribing a cough suppressant, the underlying causes of the cough, which require specific treatment, should be investigated.
If the cough does not respond to a cough suppressant administered at the usual dose, the dose must not be increased, but the clinical situation should be reassessed instead.
Mucolytic agents may induce severe bronchial congestion in infants. Infant bronchial mucus drainage capacities are limited due to the physiological characteristics of their bronchial tree. Mucolytic agents should therefore not be used in infants (see Contraindications and Adverse Reactions).
Treatment should be re-evaluated if symptoms or the disease persist or worsen.
This medicinal product contains 3.09% v/v ethanol (alcohol); i.e. up to 366 mg per tablespoon of syrup, or 1.46 g ethanol per maximum daily dose, which is equivalent to not more than 37 ml of beer or 15 ml of wine per day. Use of this medicinal product is dangerous in alcoholic subjects and the alcohol content must be taken into consideration in pregnant or breast-feeding women and high-risk groups such as patients with hepatic impairment or epilepsy.
This medicinal product contains 3 g of sucrose per measuring spoon and 9 g per tablespoon, which must be taken into account in the daily ration in case of a low sugar diet or diabetes mellitus.
Due to the presence of sucrose, patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
This medicinal product contains sodium. This medicinal product contains 13 mg of sodium per 5 ml of syrup. This should be taken into account in patients following a strict low-sodium diet.
This medicinal product contains methyl parahydroxybenzoate (E218) and may cause allergic reactions (possibly delayed).
Special warnings related to the presence of carbocisteine: Caution is recommended in the elderly, in patients with a history of gastroduodenal ulcers, and in those taking concomitant medications which may cause gastrointestinal bleeding.
If gastrointestinal bleeding occurs, patients should discontinue medication.
Warnings related to the presence of promethazine: Since phenothiazines are considered to be a potential risk factor for sudden infant death syndrome, promethazine should not be used in infants aged under 2 years (see Contraindications).
Monitoring (clinical and ECG where appropriate) should be increased in patients with epilepsy due to the possible lowering of the seizure threshold.
This medicinal product is not recommended for people 75 years of age and older.
Promethazine should be used with caution: in elderly subjects with: greater sensitivity to postural hypotension, dizziness and sedation; chronic constipation (risk of paralytic ileus); possible prostate hypertrophy,
in patients with certain cardiovascular diseases, due to the tachycardia-inducing and hypotensive effects of phenothiazines,
in patients with severe liver and/or kidney failure (due to the risk of accumulation),
in case of concomitant use of CNS depressants (due to a risk of respiratory depression).
When used in children, bronchial asthma or gastroesophageal reflux should be ruled out before using promethazine as a cough suppressant.
Intake of alcoholic beverages or medicinal products containing alcohol (see Interactions) is highly inadvisable during treatment.
Concomitant use of promethazine and sodium oxybate is not recommended (see Interactions).
Given the photosensitizing effect of phenothiazines, exposure to sun or to ultraviolet (UV) rays should preferably be avoided during treatment.
In view of its H1-antihistamine sedating properties, promethazine should be used with caution due to its risk of sedation. Combination with other sedative medicinal products should be discouraged (see Interactions).
Due to the anticholinergic properties of promethazine, the risk of severe constipation or even enterocolitis is increased when combined with other anticholinergic or neuroleptic medicinal products (see Interactions).
Effects on Ability to Drive and Use Machines: Attention is drawn especially for those who drive or use a machine, to the risk of drowsiness related to the use of this medicinal product, especially at the start of treatment.
Drinking alcohol or taking medicines that contain alcohol enhances these effects.
Use In Pregnancy & Lactation
Pregnancy: Effects related to promethazine content: Malformations (1st trimester): There is no reliable animal teratogenicity data for promethazine. In a clinical context, the use of promethazine during a limited number of pregnancies does not appear to have shown any particular teratogenic or foetotoxic effects to date. However, additional studies are necessary to evaluate the consequences of exposure during pregnancy.
Fetotoxicity (2nd and 3rd trimesters): In neonates whose mothers received long-term treatment with strong doses of an anticholinergic antihistamine such as promethazine, there have been rare reports of gastrointestinal disorders related to the atropine-like properties of phenothiazines (abdominal distention, meconium ileus, delayed meconium excretion, difficulties instituting feeding, tachycardia, neurological disorders, etc.).
In view of these data, the use of promethazine should be avoided as a precautionary measure during pregnancy. If the use of promethazine took place at the end of pregnancy, it appears to warrant monitoring of the neonate's neurological and gastrointestinal functions over a certain period.
Breast-feeding: The presence of promethazine conditions the action to be taken in case of breast-feeding.
It is not known whether promethazine passes into breast milk. Given the possibilities of sedation or paradoxical excitation in the neonate, and more so the risks of sleep apnoea evoked with phenothiazines, this medicinal product is contraindicated in breast-feeding.
Adverse Reactions
Related to the carbocisteine content: Risk of bronchial congestion, especially in infants and certain patients unable to expectorate effectively (see Contraindications and Precautions).
Allergic skin reactions such as pruritus, erythematous eruption, urticaria and angioedema.
A few cases of fixed pigmented erythema have been reported.
Gastrointestinal disorders (gastric pain, nausea, vomiting and diarrhea). If these occur, the dose should be reduced.
Gastrointestinal bleeding. Treatment should be discontinued.
Isolated cases of bullous dermatoses, such as Stevens-Johnson syndrome and erythema multiforme.
Immune system disorders: Anaphylactic/anaphylactoid reaction.
Skin and subcutaneous tissue disorders: Severe cutaneous adverse reactions (SCAR) e.g. erythema multiforme, Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN). In most of these cases reported at least one other drug was administered at the same time, which may have possibly enhanced the described mucocutaneous effects.
Related to the promethazine content: The pharmacological characteristics of this compound can cause undesirable effects that vary in severity and may or may not be dose-dependent (see Pharmacology: Pharmacodynamics under Actions).
Neurovegetative effects: sedation or drowsiness, more significant at the start of treatment; anticholinergic effects, such as dry mucous membranes, constipation, intestinal obstruction, ischemic colitis (see Precautions), accommodation disorders, mydriasis, cardiac palpitations, risk of urinary retention, orthostatic hypotension; balance disorders, dizziness, memory or concentration problems; dyskinesia, tardive dyskinesia, abnormal movements, motor incoordination, tremor (more common in the elderly), akathisia; mental confusion, hallucinations; more rarely, effects such as excitement, agitation, nervousness, insomnia.
Respiratory effects: respiratory depression.
Sensitivity reactions: erythema, eczema, pruritus, purpura, urticaria and possibly giant urticaria; oedema, in rarer cases angioedema; anaphylactic shock; photosensitization.
Hematological effects: leucopenia, neutropenia and, exceptionally, agranulocytosis; thrombocytopenia; hemolytic anemia.
Drug Interactions
The interactions mentioned are related to the promethazine content.
Atropine-like medicinal products: It should be taken into account that atropine-like substances can have additive adverse effects and more easily lead to urinary retention, acute attacks of glaucoma, constipation, dry mouth, etc.
The various atropine-like medicinal products include imipramine antidepressants, most atropine-like H1-antihistamines, anticholinergic antiparkinsonians, atropine-like antispasmodics, disopyramide, phenothiazine neuroleptics and clozapine.
Medications that lower the seizure threshold: The concomitant use of proconvulsants or medicinal products that lower the convulsive threshold should be carefully weighed because of the severity of the risk involved. These medicinal products include most antidepressants (imipramine agents, selective serotonin reuptake inhibitors), neuroleptics (phenothiazines and butyrophenones), mefloquine, chloroquine, bupropion and tramadol.
Sedative medicinal products: It should be taken into account that many medicinal products or substances can have additive depressant effects on the central nervous system and contribute to a decrease in alertness. These medicinal products include morphine derivatives (analgesics, antitussives and replacement therapies), neuroleptics, barbiturates, benzodiazepines, non-benzodiazepine anxiolytics (such as meprobamate), hypnotics, sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), sedative H1-antihistamines, centrally-acting antihypertensives, baclofen and thalidomide.
Hypnotic agents: Currently prescribed hypnotic agents are either benzodiazepines and related products (zolpidem, zopiclone), or H1-antihistamines. In addition to increased sedation when prescribed with other CNS depressants, or in the event of alcohol intake, the possible increase in the respiratory depressant effect when co-administered with morphine-like substances, other benzodiazepines, or phenobarbital should also be taken into account for benzodiazepines, especially in the elderly.
Inadvisable combinations (see Precautions): Alcohol (beverage or excipients): The sedative effect of promethazine is increased by alcohol.
Impaired alertness may make driving vehicles and using machines dangerous.
The consumption of alcoholic beverages or medicinal products containing alcohol should be avoided.
Sodium oxybate: Increased CNS depression. Impaired alertness may make driving vehicles and using machines dangerous.
Combinations requiring precautions for use: Topical agents for gastrointestinal use, antacids and adsorbents (charcoal): Decreased gastrointestinal absorption of the active ingredients.
Allow an interval (2 hours, if possible) between administration of topical gastrointestinal agents or antacids and phenothiazine neuroleptics.
Lithium: Risk of occurrence of neuropsychiatric signs suggestive of neuroleptic malignant syndrome or lithium intoxication.
Regular clinical and laboratory monitoring required, especially at the start of co-administration.
Combinations to be taken into consideration: Anticholinesterases: Risk of reduced efficacy of anticholinesterases via acetylcholine receptor antagonism due to the atropinic medicine.
Other central nervous system depressants (sedative antidepressants, barbiturates, clonidine and related, hypnotics, morphine derivatives (analgesics and antitussives), methadone, neuroleptics, anxiolytics): Increased CNS depression. Change in alertness can make driving and using machines dangerous.
Other medicinal products that lower the convulsive threshold: Increased risk of convulsions.
Atropine-like medicinal products (imipramine antidepressants, anticholinergic addition, atropine antispasmodics, disopyramide, phenothiazine neuroleptics): Addition of atropinic undesirable effects, such as urinary retention, constipation, dry mouth.
Other hypnotic agents: Increased CNS depression.
Other sedative medicinal products: Increased CNS depression. Change in alertness can make driving and using machines dangerous.
Other Orthostatic Hypotension-inducing medicinal products: Risk of increased adverse effects, particularly dizziness or syncope.
Beta-blockers in heart failure: Vasodilator effect and risk of hypotension, particularly postural (additive effect).
Dapoxetine: Risk of increased adverse effects, particularly dizziness or syncope.
Blood pressure-lowering medicinal products: Risk of increased hypotension, especially orthostatic hypotension.
Opioids: Significant risk of colonic akinesia, with severe constipation.
Orlistat: Risk of treatment failure if administered concomitantly with orlistat.
Storage
Store below 30°C.
MIMS Class
Cough & Cold Preparations
ATC Classification
R05CB10 - combinations ; Belongs to the class of mucolytics. Used in the treatment of wet cough.
Presentation/Packing
Syr (cocoa flavour) 125 mL.
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