Nap Cold

Uses

Cetirizine is used for the treatment of seasonal allergic rhinitis and conjunctivitis, perennial allergic rhinitis, pruritus and urticaria. It is also used in allergen induced asthma.

Nimesulide is used for acute pain; extra-articular disorders; osteoarthritis; post-op pain; primary dysmenorrhoea

Phenylpropanolamine is a sympathomimetic that was previously used in nasal decongestants and weight loss products, but has been withdrawn by the FDA due to safety risks and lack of efficacy.

For the treatment of nasal congestion, control of urinary incontinence, priapism and obesity.

Nap Cold is also used to associated treatment for these conditions: Chronic Idiopathic Urticaria, Flu caused by Influenza, Perennial Allergic Rhinitis (PAR), Pollen Allergy, Respiratory Allergy, Seasonal Allergic RhinitisMenstrual Distress (Dysmenorrhea), Pain, Pain, Acute, NSAIDsAllergy-Induced Respiratory Symptoms, Bronchitis, Common Cold, Cough, Nasal Congestion, Rhinorrhoea, Excess mucus or phlegm

How Nap Cold works

Cetirizine, a metabolite of hydroxyzine, is an antihistamine drug. Its main effects are achieved through selective inhibition of peripheral H1 receptors. The antihistamine activity of cetirizine has been shown in a variety of animal and human models. In vivo and ex vivo animal models have shown insignificant anticholinergic and antiserotonergic effects. In clinical studies, however, dry mouth was found to be more frequent with cetirizine than with a placebo. In vitro receptor binding studies have demonstrated no detectable affinity of cetirizine for histamine receptors other than the H1 receptors. Studies with radiolabeled cetirizine administration in the rat have demonstrated insignificant penetration into the brain. Ex vivo studies in the mouse have shown that systemically administered cetirizine does not occupy cerebral H1 receptors significantly .

The therapeutic effects of Nimesulide are the result of its complete mode of action which targets a number of key mediators of the inflammatory process such as: COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.

Phenylpropanolamine acts directly on alpha- and, to a lesser degree, 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. PPA indirectly stimulates beta-receptors, producing tachycardia and a positive inotropic effect.

Dosage

Nap Cold dosage

Tablet:

• Adults and children over 6 years: 1 tablet (10 mg) once daily or ½ tablet twice daily.
• Children 2-6 years: ½ tablet once daily.

Syrup:

• Adults and children over 6 years: 2 teaspoonful (10 mg) once daily or 1 teaspoon (5 mg) twice daily.
• Children 2-6 years: 1 teaspoonful once daily or ½ teaspoon twice daily.

100 mg twice daily.Should be taken with food. Take after meals.

Side Effects

Cetirizine dihydrochloride is well tolerated. Lower incidence of sedation, headache, dry mouth, and gastrointestinal disturbances may occur. It does not produce anticholinergic effects.

Epigastric discomfort, heartburn or abdominal cramps, nausea, vomiting and diarrhoea; skin rash, pruritus, oedema, headache, dizziness, drowsiness; hypersensitivity reactions (e.g. bronchospasm, rhinitis, angioedema urticaria); GI haemorrhage/perforation; bullous/erosive stomatitis, purpura, thrombocytopenia, toxic epidermal necrolysis, haematuria, oliguria, and renal failure; increases in liver enzymes.

Toxicity

Oral LD50 (rat): 365 mg/kg; Intraperitoneal LDLO (mouse): 138 mg/kg; Oral TDLO (rat): 50 mg/kg; Oral TDLO (mouse): 0.1 mg/kg .

Carcinogenesis and mutagenesis: In a 2-year carcinogenicity study in rats, cetirizine was not shown to be carcinogenic at dietary doses up to 20 mg/kg (approximately 15 times the maximum recommended daily oral dose in adults). In a 2-year carcinogenicity study in mice, cetirizine administration lead to an incidence of benign liver tumors in males at a dietary dose of 16 mg/kg (approximately 6 times the maximum recommended daily oral dose in adults). The clinical significance of these findings during long-term use of cetirizine is unknown at this time .

Cetirizine was not mutagenic in the Ames test, and not clastogenic in the human lymphocyte assay, the mouse lymphoma assay, and in vivo micronucleus test in rats .

Impairment of fertility

In a fertility and reproduction study in mice, cetirizine did not negatively impact fertility at an oral dose of 64 mg/kg (approximately 25 times the maximum recommended daily oral dose in adults) .

Pregnancy Category B:

In mice, rats, and rabbits, cetirizine was not teratogenic at oral doses up to 96, 225, and 135 mg/kg, respectively (approximately 40, 180 and 220 times the maximum recommended daily oral dose in adults). There are no adequate and well-controlled studies in pregnant women. Because animal studies are not always predictive of human response, cetirizine should be used in pregnancy only if clearly needed .

Use in breastfeeding/nursing

Cetirizine has been reported to be excreted in human breast milk. The use of cetirizine in nursing mothers is not recommended .

Oral TDLO (human): 1.429 mg/kg; Oral TDLO (woman): 2 mg/kg; Oral LD50 (rat): 200 mg/kg; Oral LD50 (mouse): 392 mg/kg

May induce ventricular extrasystoles and short paroxysms of ventricular tachycardia, a sensation of fullness in the head and tingling of the extremities; LD₅₀=1490mg/kg (orally in rat)

Precaution

Caution should be exercised when driving a car or operating a heavy machinery. Concurrent use of cetirizine with alcohol or other CNS depressants should be avoided because additional reduction in alertness and CNS performance may occur.

History of GI tract disease, infections, oedema, hypertension, elderly, lactation.

Interaction

No clinically significant drug interactions have been found with theophylline, azithromycin, pseudoephedrine, ketoconazole or erythromycin and with some other drugs.

Additive hepatotoxic effects with known hepatotoxins: anti-convulsants (e.g. valproic acid), anti-fungals (e.g. ketoconazole), anti-tuberculous drugs (e.g. isoniazid), tacrine, pemoline, amiodarone, methotrexate, methyldopa, amoxicillin/clavulanic acid. May decrease the oral bioavailability of furosemide and the natriuretic and diuretic response to furosemide. Increased risks of GI and hepatic adverse effects with other NSAIDs, including aspirin. May increase anti-coagulant effect of warfarin. Potentiates the action of phenytoin. May be displaced from binding sites with fenofibrate, salicylic acid, and tolbutamide. Interactions between NSAIDs and lithium, probenecid and ciclosporin, have been documented.

Volume of Distribution

Apparent volume of distribution: 0.44 +/- 0.19 L/kg .

Elimination Route

Cetirizine was rapidly absorbed with a time to maximum concentration (Tmax) of about 1 hour after oral administration of tablets or syrup formulation in adult volunteers . Bioavailability was found to be similar between the tablet and syrup dosage forms. When healthy study volunteers were given several doses of cetirizine (10 mg tablets once daily for 10 days), a mean peak plasma concentration (Cmax) of 311 ng/mL was measured .

Effect of food on absorption

Food had no effect on cetirizine exposure (AUC), however, Tmax was delayed by 1.7 hours and Cmax was decreased by 23% in the fed state .

Rapidly absorbed following oral administration.

Reduced bioavailability (about 38%) from gastrointestinal tract because of first pass metabolism by monoamine oxidase in the stomach and liver.

Half Life

Plasma elimination half-life is 8.3 hours .

1.8–4.7 hours

2.1 to 3.4 hours.

Clearance

Apparent total body clearance: approximately 53 mL/min .

Cetirizine is mainly eliminated by the kidneys , . Dose adjustment is required for patients with moderate to severe renal impairment and in patients on hemodialysis .

Elimination Route

Mainly eliminated in the urine , .

Between 70 – 85% of an orally administered dose can be found in the urine and 10 – 13% in the feces .

Renal (50%), fecal (29%)

Pregnancy & Breastfeeding use

Pregnancy category B. There are no adequate and well controlled studies in pregnant women. Cetirizine should be used during pregnancy only if clearly needed. Cetirizine has been reported to be excreted in human breast milk. As large amount of drugs are excreted in human milk, use of Cetirizine in nursing mother is not recommended.

Category not classified

Contraindication

Cetirizine Dihydrochloride is contraindicated in those patients with a known hypersensitivity to it or any of its ingredients or hydroxyzine.

Hypersensitivity; GI bleeding, active peptic ulcer disease; severe renal and heart failure; hepatic impairment or known liver disease; coagulation disorders; pregnancy; children <12 yr.

Acute Overdose

Symptoms: Confusion, dizziness, fatigue, headache, malaise, restlessness, sedation, somnolence, diarrhoea, mydriasis, pruritus, stupor, tachycardia, tremor, and urinary retention.

Management: Symptomatic and supportive treatment. Gastric lavage may be done shortly following ingestion.

Epigastric pain, nausea, vomiting, drowsiness, lethargy, GI haemorrhage, seizures, hypertension, apnoea, coma, anaphylactic reactions and renal failure. Treatment is supportive.

Storage Condition

Store between 20-25°C. Syrup: Store between 2-8°C.

Protect from heat and humidity; store at <25°C.

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