Drug Interaction:
Antihistamines Include:
First Generation ( Non-selective )
Ethanolamine- Carbinoxamine. Clemastine, Diphenhydramine.
Ethylenediamines- Pyrilamine, Triplennamine
Akylamines- Brompheneramine, Chlorpheniramine, Dexchlor pheniramine,Pheniramine,
Triprolidine
Phenothiazines- Methidilazine, Promethizine, trimeprazine
Piperidines- Azatadine, Cyproheptadine, Phenindamine
Miscellaneous- Astemazole, Loratadine, Terfenadine
Second Generation ( Peripherally selective )
Phthalazinone - Azelastine
Piperazine - Cetrizine
Refer - Chlorpheniramine maleate
CNS depressants. Alcohol,
May be potentiated by theophylline
Indication:
Perennial and seasonal rhinitis
Urticaria
Perennial and seasonal rhinitis
Urticaria
Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
1.Cetrizine Hcl- June 1993
Seasonal rhinitis perennial allergic rhinitis pruritus
2.Cetrizine 10mg + Ambroxol 75mg sr 13-04-2009
tablet
For symptomatic relief of productive cough associated with
allergic rhinitis, when both anti-histamine and mucolytic
agents are desired
3. Cetrizine 5/10mg+ Ambroxol 30mg 23-02-2009
per 5 ml syrup
For the symptomatic relief of productive cough associated with
allergic rhinitis, when both anti-histamine and muculytic agents
are desired
FIXED DOSE COMBINATIONS APPROVED BY DCG(I)
FROM JANUARY 1961 TILL NOVEMBER 2014
Name of Drug Indication Date of Approval
1.Cetrizine Dihydrochloride 5mg (immediate release)+ 09-09-1997
Pseudoephedrine Hcl 120mg SR tablet
For the treatment of seasonal allergic rhinitis
2.Combi kit of 5 tablets each 01-08-2004
i. Pseudoephedrine Hcl 120mg ER +
Cetrizine Hcl 5mg (orange tablet) and
ii. Pseudoephedrine HCL ER 120mg +
Tripolidine 2.5mg (Blue tablets)
For the treatment of symptomatic relief of allergic rhinitis in
adults only
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Cetrizine Respiratory Pfizer Inc. 25-06-2007
Antihistamines Include:
First Generation ( Non-selective )
Ethanolamine- Carbinoxamine. Clemastine, Diphenhydramine.
Ethylenediamines- Pyrilamine, Triplennamine
Akylamines- Brompheneramine, Chlorpheniramine, Dexchlor pheniramine,Pheniramine,
Triprolidine
Phenothiazines- Methidilazine, Promethizine, trimeprazine
Piperidines- Azatadine, Cyproheptadine, Phenindamine
Miscellaneous- Astemazole, Loratadine, Terfenadine
Second Generation ( Peripherally selective )
Phthalazinone - Azelastine
Piperazine - Cetrizine
Refer - Chlorpheniramine maleate
Adverse Reaction:
Drowsiness, headache, dry mouth, dizziness, agitation, GI upset
Aggressive reaction, convulsions, somnolence, fatigue, pharyngitis,
Arthalgia,
Children- also diarrhea
Bronchospasm, cough, epistaxis, irritability, insomnia
Contra-Indications:
Hypersensititivity, to hydroxzine,
Pregnancy.actation
Special Precauton-
Elderly, hepatic , renal impairment,
Dosages/ Overdosage Etc:
Indication-
Perennial and seasonal rhinitis
Urticaria
Dosage- Adults and children over 6 years - 10mg daily
Other Information:
For Availability/supplies
Contact -
1.Indian Drug Manufacturers Association (IDMA)
Phone- 022- 24944624/ 24974308
Fax- 022- 24950723
Email- idma@vsnl.com
Website: www.idma-assn.org
2.Bulk Drug Manufacturers Association (India)(BDMA)
Phone - 040-23703910/ 23706718
Fax- 040-23704804
Email- info@bdmai.org
Website: www.info@bdmai.org
Pharmacology/ Pharmacokinetics:
Ref- Drug Facts And Comparisons(2010)
Refer antihistamines
Peripherally Selective H1 Antagonists- include-
Cetrizine, Desloradine, Fexofenadine, Loratidine-
Refer Cetrizine
Pharmacokinetics-
Cetrizine is a metabolite of hydroxyzine . Desloradine is a metabolite of loratidine. The
pharmacokinetics of second-generation agents have been studied more throughly and
are provided in the table below-
Pharmacokinetics of Peripherally Selective H1 antagonists
Parameters
Onset of Action Tmax Elimination Protein CYP450 Food effect
h t 1/2 binding metabolism of absptn
h %
Drug
Cetrizine
rapid 1 8.3 93 50% excreted delayed 1.7h
unchanged
Desloratadine
<1h 3 27 82-87 - none
Fexofenadine
rapid 2.6 14.4 60-70 95% excreted -
unchanged
Loratadine
rapid 1.3 to 2.5 8.4to 28 97(75) inc 3A4, 2D6 delayed 1h
Interaction with Food:
Reduction in rate but not extent of absorption
Pregnancy and lactation:
Use contraindicated. Observe caution
Manufacturer Details