Each CARINOX capsule contains 5mg Loratadine and 120mg Pseudoephedrine
Sulphate. CARINOX are size 0 capsules which has an ivory (opaque) body and a
rich yellow (opaque) cap with 'CARINOX' printed on both cap and body of the
Gelatin for capsule : Bovine source certified with Halal certification.
CARINOX capsules are indicated for the relief of symptoms associated with
allergic rhinitis and the common cold including nasal congestion, sneezing,
rhinorrhea, pruritus and lacrimation.
ACTIONS AND MODE OR MECHANISMS OF ACTION
Loratadine is a potent long-acting tricyclic antihistamine with selective
peripheral Ht-receptor antagonistic activity.
Pseudoephedrine sulfate, one of the naturally occurring alkaloids of the
Ephedra and an orally administered vasoconstrictor, produces a gradual but
sustained decongestant effect facilitating shrinkage of congested mucosa in
upper respiratory areas.
The mucuos membrane of the respiratory tract is decongested through the
action of the sympathetic nerves.
PHARMACOLOGY (SUMMARY OF PHARMACODYNAMIC AND PHARMACOKINETIC(S)
Loratadine is rapidly absorbed from the gastro-intestinal tract after oral
administration, peak plasma concentrations being attained in about one hour.
Bioavailability is increased and time to peak plasma concentrations is
delayed when administered with food. Loratadine undergoes extensive
The major metabolite, descarboethoxyloratadine, has potent histamine-H1
blocking activity. Reported half-lives for loratadine and
descarboethoxyloratadine are 12 and 18 hours respectively. Loratadine is
about 98% bound to plasma proteins; descarboethoxyloratadine is less
extensively bound. Loratadine and its metabolites have been detected in
breast milk, but do not appear to cross the blood brain barrier to a
significant extent. Loratadine and its metabolites are excreted in the urine
Pseudoephedrine is absorbed from the gastro-intestinal tract. It is
resistant to metabolism by monoamine oxidase and is largely excreted
unchanged in the urine together with small amounts of its hepatic
metabolite. It has a half-life of several hours; elimination is enhanced and
half-life accordingly shorter in acid urine. Small amounts are excreted in
RECOMMENDED DOSAGE, DOSAGE SCHEDULE AND ROUTE OF ADMINISTRATION
Adults and children 12 years of age and over: One CARINOX capsule twice a
SYMPTOMS AND TREATMENT FOR OVERDOSAGE, AND ANTIDOTE(S)
In the event of overdosage, general symtomatic and supportive treatment
should be started immediately and maintained for as long as necessary.
They may vary from CNS depression (sedation, apnea, diminished mental
alertness, cyanosis, coma, cardiovascular collapse) to stimulation
(insomnia, hallucination, tremors or convulsions) to death. Other signs and
symptoms may be euphoria, excitement, tachycardia, palpitations, thirst,
perspiration, nausea, dizziness, tinnitus, ataxia, blurred vision and
hypertension or hypotension. Stimulation is particularly likely in children,
as are atropine-like signs and symptoms (dry mouth; fixed, dilated pupils;
flushing; hyperthermia; and gastro-intestinal symptoms).
In large doses sympathomimetics may give rise to giddiness, headache,
nausea, vomiting, sweating, thirst, tachycardia, precordial pain,
palpitations, difficulty in micturition, muscular weakness and tenseness,
anxiety, restlessness and insomnia. Many patients can present a toxic
psychosis with delusions and hallucinations. Some may develop cardiac
arrhythmias, circulatory collapse, convulsions, coma and respiratory
failure. The oral LD50 values for this combination product were greater than
525 and 1839 mg/kg in mice and rats, respectively.
The patient should be induced to vomit, even if emesis has occurred
spontaneously. Pharmacologically-induced vomiting by the administration of
ipecac syrup is a preferred method. However, vomiting should not be induced
in patients with impaired consciousness. The action of ipecac is facilitated
by physical activity and by the administration of 240 to 360 mililitres of
water. If emesis does not occur within 15 minutes, the dose of ipecac should
be repeated. Precautions against aspiration must be taken, especially in
Following emesis, absorption of any drugs remaining in the stomach may be
attempted by the administration of activated charcoal as a slurry with
water. If vomiting is unsuccessful, or contraindicated, gastric lavage
should be performed. Physiologic saline solution is the lavage solution of
choice, particularly in children. In adults, tap water can be used; however,
as much as possible of the amount administered should be removed before the
next instillation. Saline cathartics draw water into the bowel by osmosis
and therefore may be valuable for their action in rapid dilution of bowel
content. It is not known whether this is dialyzable. After emergency
treatment, the patient should continue to be medially monitored.
Treatment of the signs and symptoms of overdosage is symptomatic and
supportive. Stimulants(analeptic agents) should not be used. Vasopressors
may be used to treat hypotension. Short-acting barbiturates, diazepam, or
paraldehyde may be administered to control seizures. Hyperpyrexia,
especially in children, may require treatment with tepid water sponge baths
or hypothermic blanket. Apnea is treated with ventilatory support.
CARINOX capsules are contraindicated in patients who hale shown
hypersensitivity or idiosyncrasy to their components, to adrenergic agents
or to other drugs of similar chemical structure. CARINOX capsules also are
contraindicated in patients receiving MAO therapy or within fourteen days of
discontinuing such treatment and in patients with narrow angle glaucoma,
urinary retention, severe hypertension,
severe coronary artery disease and hyperthyroidism.
PRECAUTIONS / WARNINGS
Sympathomimetics should be used with caution in patients with glaucoma,
stenosing peptic ulcer, pyloroduodenal obstruction, prostatic hyperthrophy
or bladder neck obstruction, cardiovascular disease, increased intraocular
pressure or diabetes mellitus. Sympathomimetics should be used with caution
in patients receiving digitalis. Sympathomimetics may cause central nervous
system (CNS) stimulation, excitability, convulsions, and/or cardiovascular
collapse with accompanying hypotension. In patients 60 years of age or
older, sympathomimetics are also more likely to cause adverse reactions such
as confusion, hallucination, convulsions, CNS depression and death.
Consequently, caution should be exercised when administering a repeat-action
formulation to elderly patients.
Patients with severe liver impairment should be administered a lower initial
dose because they may have reduced clearance of loratadine; an initial dose
of one tablet daily is recommended.
Drug Abuse and Dependence:
There is no data available to indicate that abuse or dependency occurs with
Pseudoephedrine sulfate, like other CNS stimulants, has been abused. At high
doses, subjects commonly experience an elevation of mood, decreased appetite
and a sense of increased physical energy, mental capacity and alertness.
Anxiety, irritability and loquacity also have been experienced. With
continued use, tolerance develops; the user increases the dose and
ultimately toxicity occurs. Depression may follow rapid withdrawal.
Safety and Efficacy of CARINOX capsules in children younger than 12 years of
age have not been established.
Usage during Pregnancy and in nursing Mothers:
Safe use of CARINOX capsules during pregnancy has not been established.
Therefore, the product should be used only if potential benefit justifies
the potential risk to the foetus. Since loratadine and pseudoephedrine
sulphate are excreted in breast milk, a decision should be made whether to
discontinue nursing or discontinue the use of this product.
SIDE EFFECTS / ADVERSE REACTIONS
During controlled clinical studies with the recommended dosage, the
incidence of adverse effects associated with CARINOX was comparable to that
of placebo, with the exception of insomnia and dry mouth, both of which were
commonly reported. Other reported adverse reactions associated with both
CARINOX and placebo included headache and somnolence.
Rare adverse reactions in decreasing order of frequency included
nervousness, dizziness, fatigue, nausea, abdominal distress, thirst,
anorexia, tachycardia, pharyngitis, rhinitis, acne, pruritus, rash,
urticaria, arthralgia, confusion, dysphonia, hyperkinesia, hypoesthesia,
decreased libido, paraesthesia, tremor, vertigo, flushing, postural
hypotension, increased sweating, eye disorders, earache, tinnitus, taste
abnormality, agitation, apathy, depression, euphoria, paroneiria, increased
appetite, change in bowel habits, dyspepsia, eructation, hemorrhoids, tongue
discolouration, tongue disorder, vomiting, transient abnormal hepatic
function, dehydration, increased weight, hypertension, palpitation,
migraine, bronchospasm, coughing, dyspnea, epitaxis, nasal congestion,
sneezing, nasal irritation, dysuria, micturition disorder, nocturia, urinary
retention, asthenia, back pain, leg cramps, malaise and rigors.
During the marketing of loratadine, alopecia, anaphylaxis and abnormal
hepatic function have been reported rarely.
When administered concomitantly with alcohol, loratadine has no potentiating
effects as measured by psychomotor performance studies.
Increased plasma concentrations of loratadine have been reported after
concomitant use with ketoconazole, erythromycin or cimetidine in controlled
clinical trials, but without clinically significant changes (including
electrocardiographic). Other drugs known to inhibit hepatic metabolism
should be coadministered with caution until definitive interactions studies
can be completed.
When sympathomimetics are given to patients receiving monoamine oxidase
(MAO) inhibitors, hypertensive reactions, including hypertensive crises may
occur. The antihypertensive effects of methyldopa, mecamylamine, reserpine
and veratum alkaloids may be reduced by sympathomimetics. Beta-adrenergic
blocking agents may also interact with sympathomimetics. Increased ectopic
pacemaker activity can occur when pseudoephedrine is used concomitantly with
digitalis. Antacids increase the rate of pseudoephedrine absorption; kaolin
Drug/Laboratory Test Interactions:
Antihistamines should be discontinued approximately 48 hours prior to skin
testing procedures since anthistamines may prevent or diminish otherwise
positive reactions to dermal reactivity indicators.
The in vitro addition of pseudoephedrine to sera containing the cardiac
isoenzyme MB of serum creatinine phosphokinase progressively inhibits the
activity of the enzyme. The inhibition becomes complete over six hours.
PACKING / PACK SIZE
CARINOX is supplied in cartons of 10's, 100's, 500's and 1000's
STORAGE CONDITIONS, USER INSTRUCTIONS, AND PHARMACEUTICAL PRECAUTIONS
Store in a dry place below 30°C.
Protect from excessive moisture.