Ximelagatran/Melagatran: a review of its use in the prevention of venous thromboembolism in orthopaedic surgery.

Unlabelled: Ximelagatran (Exanta), the first available oral direct thrombin inhibitor, and its active form, melagatran, have been evaluated in the prevention of venous thromboembolism (VTE) in patients undergoing hip or knee replacement. After oral administration ximelagatran is rapidly bioconverted to melagatran. Melagatran inactivates both circulating and clot-bound thrombin by binding to the thrombin active site, thus, inhibiting platelet activation and/or aggregation and reducing fibrinolysis time.

Pantoprazole: an update of its pharmacological properties and therapeutic use in the management of acid-related disorders.

Pantoprazole (Protonix) is an irreversible proton pump inhibitor (PPI) that reduces gastric acid secretion. In combination with two antimicrobial agents (most commonly metronidazole, clarithromycin or amoxicillin) for 6-14 days, pantoprazole 40 mg twice daily produced Helicobacter pylori eradication rates of 71-93.8% (intent-to-treat [ITT] or modified ITT analysis) in patients without known antibacterial resistance.

Anastrozole: in early breast cancer.

Anastrozole, a nonsteroidal selective aromatase inhibitor, has recently been approved in the US and several other countries for the adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer. In the Arimidex, Tamoxifen alone or in Combination (ATAC) trial, anastrazole 1mg was significantly more effective than tamoxifen 20mg or combined treatment (17 and 19% relative risk reduction) for disease-free survival in postmenopausal women with early breast cancer. black triangle Anastrazole was also significantly more effective than tamoxifen for time to tumour recurrence and the odds of a primary contralateral tumour as a first event.

Gefitinib.

Gefitinib (ZD1839) is an orally active selective inhibitor of epidermal growth factor receptor tyrosine kinase, an enzyme that regulates intracellular signalling pathways implicated in the proliferation and survival of cancer cells. In human non-small cell lung cancer (NSCLC) cell lines and xenografts, gefitinib dose-dependently inhibited cellular proliferation and tumour growth, and potentiated the cytotoxic effects of chemotherapy and/or radiation. Gefitinib is orally bioavailable and is cleared via the cytochrome P450 3A4 pathway.

Valsartan/hydrochlorothiazide: a review of its pharmacology, therapeutic efficacy and place in the management of hypertension.

Unlabelled: The combination of valsartan [an angiotensin II type 1 (AT(1)) receptor blocker] and hydrochlorothiazide (a thiazide diuretic), administered once daily, has been evaluated in the treatment of patients with hypertension in clinical trials ranging in duration from 8 weeks to 3 years. These studies showed that combination treatment with valsartan 80 or 160mg and hydrochlorothiazide 12.5 or 25mg induced significant reductions from baseline in systolic blood pressure (SBP) and diastolic BP (DBP) in patients with mild to severe hypertension.

Airmax: a multi-dose dry powder inhaler.

Airmax is a multi-dose dry powder inhaler. An internal pump measures out the drug dose using controlled air pressure. Inhalation transports the drug into a cyclone separator (where active drug is separated from the lactose carrier) and then into the patient airway.

Tamsulosin: a review of its pharmacology and therapeutic efficacy in the management of lower urinary tract symptoms.

Unlabelled: Tamsulosin is a subtype-selective alpha(1A)- and alpha(1D )-adrenoceptor antagonist. alpha(1)-Receptors predominate in the prostate gland, prostatic capsule, prostatic urethra and bladder, and the relaxation of prostate and bladder smooth muscles is associated with improved maximal urine flow (Q(max)) and alleviation of lower urinary tract symptoms (LUTS) in patients with benign prostatic hyperplasia (BPH). Tamsulosin 0.

Interleukin-2. A review of its pharmacological properties and therapeutic use in patients with cancer.

Recombinant interleukin-2 (IL-2) products (e.g. aldesleukin, teceleukin) are nonglycosylated, modified forms of the endogenous compound.

Cyclosporin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in immunoregulatory disorders.

Cyclosporin is a lipophilic cyclic polypeptide which produces calcium-dependent, specific, reversible inhibition of transcription of interleukin-2 and several other cytokines, most notably in T helper lymphocytes. This reduces the production of a range of cytokines, inhibiting the activation and/or maturation of various cell types, including those involved in cell-mediated immunity. Thus, cyclosporin has immunosuppressive properties, and has a proven place as first line therapy in the prophylaxis and treatment of transplant rejection.