CEZINE

Indications

• Chronic idiopathic urticaria
• Perennial allergic rhinitis
• Seasonal allergic rhinitis
• Allergic asthma
• Physical urticaria
• Atopic dermatitis

Dosage

Children: For children aged 6 to 12 years, the dosage is typically 5 mg to 10 mg once daily depending on the severity of symptoms. For children aged 2 to 6 years, the usual dose is 2.5 mg to 5 mg once daily. Specific dosing should refer to the BNF for Children.

Adults: The typical adult dose is 10 mg once daily, which can be adjusted based on the severity of symptoms and patient response.

Mechanism of action

Cetirizine selectively inhibits peripheral H1 receptors, effectively blocking the action of histamine, which is responsible for allergic symptoms. It has demonstrated negligible anticholinergic and antiserotonergic effects, and studies indicate minimal penetration into the central nervous system, reducing the likelihood of sedation.

Pharmacodynamics

Cetirizine exhibits antihistaminic activity that effectively minimizes or eliminates symptoms of various allergic conditions such as chronic idiopathic urticaria and allergic rhinitis. It has anti-inflammatory properties that may assist in asthma management and can significantly reduce the duration and dosage of topical anti-inflammatory treatments for conditions like atopic dermatitis. Its effects can be observed within 20 minutes of administration, lasting up to 24 hours.

Pharmacokinetics

Cetirizine is well absorbed orally with peak plasma concentrations occurring approximately 1 hour after dosing. It has a half-life of about 8 hours, allowing for once-daily dosing in most cases. The drug is primarily excreted in the urine, with minimal hepatic metabolism, making it suitable for patients with liver impairment.

Adverse effects

• dry mouth
• drowsiness
• fatigue
• headache
• nausea

Precautions

• Use with caution in patients with renal impairment
• Caution advised in individuals with a history of seizures

Pregnancy

Cetirizine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Cetirizine is excreted in breast milk; caution is advised when administered to breastfeeding mothers.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• tablets
• oral solution
• syrup

Indications

• Moderate to severe pain management
• Cough suppression

Dosage

Children: Refer to the BNF for Children for appropriate dosing recommendations in pediatric patients.

Adults: Refer to the BNF for specific dosing guidelines as it varies based on the formulation and patient factors.

Mechanism of action

Dihydrocodeine acts primarily as an agonist at the mu-opioid receptors in the central nervous system. This interaction leads to the inhibition of pain pathways, resulting in the alleviation of pain. Additionally, it may interact with other opioid receptors, contributing to its overall analgesic effect.

Pharmacodynamics

The analgesic effects of dihydrocodeine typically manifest within 30 to 60 minutes after administration, peaking within a few hours. Its effects may last for 4 to 6 hours, depending on the formulation and individual patient factors. Dihydrocodeine can also produce sedation and euphoria, as well as respiratory depression, which are common effects associated with opioid use.

Pharmacokinetics

Dihydrocodeine is absorbed well from the gastrointestinal tract, with an oral bioavailability of approximately 25% due to first-pass metabolism. It is metabolized primarily in the liver, with the cytochrome P450 system playing a significant role in its conversion to active metabolites. The elimination half-life of dihydrocodeine is approximately 3 to 4 hours, and it is excreted mainly in the urine as metabolites.

Adverse effects

• Dizziness
• Headache
• Nausea
• Vomiting
• Dry mouth
• Constipation
• Drowsiness

Precautions

• Use with caution in patients with a history of drug abuse
• Caution in patients with hepatic or renal impairment
• Monitor for signs of respiratory depression
• Use with caution in elderly patients

Pregnancy

Safety in pregnancy has not been established, use only if clearly needed.

Breast-feeding

It is not known if dihydrochloride is excreted in human milk, caution is advised.

Storage

Store in a cool, dry place, away from light. Keep out of reach of children.

Mechanism of action

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. Cetirizine, a human metabolite of hydroxyzine, is an antihistamine; its principal effects are mediated via selective inhibition of peripheral H1 receptors. The antihistaminic activity of cetirizine has been clearly documented in a variety of animal and human models. In vivo and ex vivo animal models have shown negligible anticholinergic and antiserotonergic activity. In clinical studies, however, dry mouth was more common with cetirizine than with placebo. In vitro receptor binding studies have shown no measurable affinity for other than H1 receptors. Autoradiographic studies with radiolabeled cetirizine in the rat have shown negligible penetration into the brain. Ex vivo experiments in the mouse have shown that systemically administered cetirizine does not significantly occupy cerebral H1 receptors.

Pharmacodynamics

**General effects and respiratory effects** Cetirizine, the active metabolite of the piperazine H₁-receptor antagonist hydroxyzine, minimizes or eliminates the symptoms of chronic idiopathic urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, allergic asthma, physical urticaria, and atopic dermatitis. The clinical efficacy of cetirizine for allergic respiratory diseases has been well established in numerous trials. **Effects on urticaria/anti-inflammatory effects** It has anti-inflammatory properties that may play a role in asthma management. There is evidence that cetirizine improves symptoms of urticaria. Marked clinical inhibition of a wheal and flare response occurs in infants, children as well as adults within 20 minutes of one oral dose and lasts for 24 h. Concomitant use of cetirizine reduces the duration and dose of topical anti-inflammatory formulas used for the treatment of atopic dermatitis.