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ZYRTEC® UCB Pharma Cetirizine HCl Histamine H1-Receptor Antagonist Action And Clinical Pharmacology: Cetirizine, a human metabolite of hydroxyzine, is a histamine H1 receptor antagonist antiallergic compound; its principal effects are mediated via selective inhibition of peripheral H1 receptors. Cetirizine is distinguished from other histamine H1 receptor antagonists by the presence of a carboxylic acid function. This difference may be partly responsible for the selectivity of cetirizine seen in pharmacologic models…

ZOVIRAX® Oral Glaxo Wellcome Acyclovir Antiviral Agent Action And Clinical Pharmacology: See Zovirax Cream. During suppression therapy there is no evidence that acyclovir prevents neural migration of the virus. It aborts episodes of recurrent herpes due to inhibition of viral replication following reactivation. Pharmacokinetics: The pharmacokinetics of acyclovir after oral administration have been evaluated in 6 clinical studies involving 110 adult patients. In one study of 35 immunocompromised patients with…

ZOVIRAX® Cream Glaxo Wellcome Acyclovir Antiviral Agent Action And Clinical Pharmacology: Acyclovir, a synthetic acyclic purine nucleoside analog, is a substrate with a high degree of specificity for herpes simplex and varicella-zoster specified thymidine kinase. Acyclovir is a poor substrate for host cell-specified thymidine kinase. Herpes simplex and varicella-zoster specified thymidine kinase transform acyclovir to its monophosphate which is then transformed by a number of cellular enzymes to acyclovir diphosphate…

ZYLOPRIM® Glaxo Wellcome Allopurinol Xanthine Oxidase Inhibitor Action And Clinical Pharmacology: Allopurinol is a structural analogue of hypoxanthine. Reduction in both the serum and urinary uric acid levels is brought about by allopurinol inhibiting the action of xanthine oxidase, the enzyme responsible for the conversion of hypoxanthine to xanthine and xanthine to uric acid. Allopurinol is metabolized to the corresponding xanthine analogue, oxypurinol, which is also an inhibitor of xanthine…

ZYPREXA® Lilly Olanzapine Antipsychotic Action And Clinical Pharmacology: Pharmacodynamics: Olanzapine, a thienobenzodiazepine, is an antipsychotic agent, displaying high receptor affinity binding in vitro at serotonin 5-HT2A/C (Ki=4 and 11 nM, respectively), dopamine D1, D2, D3, D4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9 to 2.5 nM), adrenergic a1(Ki=19 nM), and histamine H1 (Ki=7 nM) receptors. In a behavioral paradigm predictive of antipsychotic activity, olanzapine reduced conditioned avoidance response in rats…

ZOSTRIX® H.P. Medicis Capsaicin Neuralgia Therapy Action And Clinical Pharmacology: Current evidence suggests that capsaicin works by its action on a pain transmitting compound called substance P. Capsaicin causes substance P to leave the nerve endings. With a lower amount of substance P in the nerve endings, pain impulses cannot be transmitted to the brain. Indications: For the relief of neuralgias (pain from nerves near the surface of the skin)…

ZOSTRIX® Medicis Capsaicin Neuralgia Therapy Action And Clinical Pharmacology: Although the precise mechanism of action of capsaicin is not fully understood, current evidence suggests that capsaicin renders skin insensitive to pain by depleting and preventing reaccumulation of substance P in peripheral sensory neurons. Substance P is thought to be the principal chemomediator of pain impulses from the periphery to the CNS. Indications: For the temporary relief of the pain (neuralgia)…

ZOVIRAX® for Injection Glaxo Wellcome Acyclovir Sodium Antiviral Agent Action And Clinical Pharmacology: Acyclovir, a synthetic acyclic purine nucleoside analog, is a substrate with a high degree of specificity for herpes simplex and varicella-zoster-specified thymidine kinase. Acyclovir is a poor substrate for host cell-specified thymidine kinase. Herpes simplex and varicella-zoster-specified thymidine kinase transform acyclovir to its monophosphate which is then transformed by a number of cellular enzymes to acyclovir diphosphate…

ZOVIRAX® Ointment Glaxo Wellcome Acyclovir Antiviral Agent Action And Clinical Pharmacology: Acyclovir, an acyclic nucleoside analog, is a substrate specific for herpesvirus-specified thymidine kinase. It inhibits replication of these viruses. Normal cellular thymidine kinase does not effectively utilize acyclovir as a substrate. Herpes-virus-specified thymidine kinase transforms acyclovir to its monophosphate which is then transformed by cellular enzymes to acyclovir diphosphate and acyclovir triphosphate. Acyclovir triphosphate is both an inhibitor of,…