Antihistamines in the dog and cat

Antihistamines may be used to inhibit H1 receptors in pruritic dermatoses in dogs and cats.
They are rarely effective as a monotherapy for pruritus because of the multiple other
mechanisms of itch independent of histamine. They may have some steroid sparing properties.
The bioavailability and receptor affinity of antihistamines in the dog and cat are often not known
and as such dose rates recommended are often anecdotal.
When we use antihistamines it is generally in conjunction with initiation of immunotherapy for
atopic dermatitis. We will commonly use them in combination with essential fatty acids and/or
corticosteroids to minimise the reliance on corticosteroids. The pharmacologic response to
antihistamines relies on tissue distribution and receptor occupancy PLUS non H1 receptor
mediated mechanisms (depending on the antihistamine used), so we will often trial several
antihistamines for 7-10 days each. If there is a possible reduction in itch then there should be a
4 day washout in between trials. We will have to rely on owners subjective perception of
efficacy in controlling pruritus.
Recently hydroxyzine has been shown to have good bioavailability in the dog when given at
2mg/kg. An older pharmacokinetic study of chlorpheniramine in dogs suggests that much higher
doses than those traditionally recommended are required to achieve significant bioavailability.
Even less is known about the bioavailability of antihistamines in cats but anecdotally the
efficacy is considered slightly better than in dogs. Our most reliable antihistamine in cats is
Zyrtec 5mg/cat.
Suggested dose rates for dogs are as follows:
Hydroxyzine (2mg/kg q12h) *
Chlorpheniramine (0.1-0.5 mg/kg q8-12h) *
Polaramine (dexchlorpheniramine, 0.1-0.5 mg/kg q12h, max 6mg dose) *
Histalert (diphenylpyraline, 0.1-0.2 mg/kg q12h) *
Phenergan (promethazine, 1-2 mg/kg q12h) *
Periactin (cyproheptadine, 0.1-0.5 mg/kg q12h) *
Claratyne (loratidine, 0.5 mg/kg q24h)
Claramax (desloratidine, 10mg/20kg dog q24h)
Xergic (fexofenedine, 60mg/10-20kg q24h)
Zyrtec (cetirizine, 1mg/kg q24h)
* First generation antihistamines
Side effects are uncommon with antihistamines but include sedation, constipation, dry gums
and anxiety. These are more common with the first generation antihistamines. Concurrent use
of P-glycoprotein (PGP) inhibitors (which includes some antihistamines) may increase the risk
of sedation with Claratyne, Xergic, and Zyrtec. Antihistamines that are PGP inhibitors may also
increase the penetration of the blood brain barrier of other drugs that are PGP substrates (such
as amitriptyline, ivermectin, chlorpromazine, cyclosporin, digoxin and loperamide) and
concurrent use of these is not normally recommended.
Some commonly used P-glycoprotein inhibitors
Cyclosporin, Cyproheptadine (Periactin), Fentanyl, Fluoxetine, Hydroxyzine, Ketoconazole,
Itraconazole, Ivermectin, Levothyroxine, Loratidine (Claratyne), Ofloxacin, Promethazine (Phenergan),
Terfenedine (Teldane)

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