Pocket Drug Guide

Posts Tagged ‘Indication Treatment’

Brand Name Drug: Relpax
Active Ingredient Drug:  eletriptan
Indication: Treatment of symptoms of acute migraine headache
Company Name:  Pfizer Inc

Introduction

During a migraine headache attack, brain activity changes induce inflammation of cerebral blood vessels and nerves. Attacks may be triggered by alcohol, certain foods, too much or too little sleep, menstruation, emotional stress, or environmental factors. Sumatriptan was the first serotonin agonist for treating migraine, but a new faster, more effective antimigraine drug: Relpax (eletriptan). Manufactured by Pfizer Inc., Relpax is also a serotonin agonist but its affinity for these receptors is different from that of sumatriptan.

How It Works

The triptan antimigraine drugs are derived from the serotonin molecule. They act on 5-hydroxytryptamine (HT) 1B/1D receptors on blood vessels, trigeminal neurons, and the trigeminal nucleus caudalis, causing constriction of extracerebral intracranial vessels, abolition of dural extravasation and neurogenic inflammation, and inhibition of trigeminal neuronal discharge. Relpax has more than a 6-fold higher affinity than sumatriptan at the 5-HT1D receptor and more than a 3-fold greater affinity at the 5-HT1B receptor. Relpax also binds potently to the 5-HT1F receptor.

Relpax: Clinical Study Results

One study compared the efficacy of Relpax with that of sumatriptan and placebo in 692 patients who suffered from migraine headaches. Subjects were randomized to receive oral Relpax (20 mg, 40 mg, or 80 mg), sumatriptan 100 mg, or placebo. Within 1 hour of administration, pain was reportedly reduced from moderate-severe to mild-none in 24% of those taking 20 mg Relpax, 38% of those taking 40 mg Relpax, and 41% of patients taking 80 mg Relpax, compared to 20% of patients taking 100 mg sumatriptan and 12% of subjects taking placebo – a significant difference. At 2 hours, 77% of the Relpax group reported mild/no pain versus 55% of the sumatriptan group, while at 4 hours the corresponding values were 58% for Relpax and 46% for sumatriptan. Patient acceptability was 64% for 100 mg sumatriptan and 20 mg Relpax, 74% for 40 mg Relpax, and 84% for 80 mg Relpax, indicating that 80 mg of Relpax is the dose that patients preferred most.

Another study showed that Relpax is as effective in treating migraine during menstruation as it is during non-menstruation. A group of 454 women with migraine received 20 mg, 40 mg, or 80 mg Relpax, 100 mg of sumatriptan, or placebo. The results showed that 41% to 71% of women taking Relpax for a menstrually-related migraine reported a reduction in headache pain from moderate-severe to mild-none at 2 hours, as did 55% to 76% of women taking Relpax who were not menstruating. For sumatriptan, the 2-hour headache response was 54%. None of the results differed significantly from each other.

What the Patient Should Know

Adverse side effects associated with serotonin agonists include warmth and tingling, dizziness, nausea or vomiting, and chest or throat pain or tightness. As with all drugs, the patient should inform his or her healthcare provider of any other medications being taken, since serotonin agonists may interact with certain antidepressants and other medications.

Brand Name: Zometa
Active Ingredient: Zometa
Indication: Treatment of tumor-induced hypercalcemia
Company Name: Novartis Pharmaceuticals Corporation

Introduction

Tumor-induced hypercalcemia (TIH) most commonly develops in patients with advanced breast cancer, multiple myeloma, non-small cell lung cancer, and prostate cancer, and often occurs as a complication of bone metastases. TIH is potentially life-threatening, usually occurring late in malignancy and limiting survival. Signs and symptoms of tumor-induced hypercalcemia include nausea, vomiting, dehydration, renal insufficiency, mental confusion, and extremely high serum calcium levels (greater than 10.5 mg/dl).

How It Works

Cancer can accelerate the breakdown of bone, leading to tumor-induced hypercalcemia. Zometa is a biphosphonate that works by inhibiting osteoclastic bone resorption, the process by which calcium is released into the bloodstream. It is believed that biphosphonates become incorporated into bone matrix and are imbibed by osteoclasts during resorption, incapacitating the osteoclast and decreasing resorption.

Zometa: Clinical Study Results

Two clinical studies compared Zometa to Aredia (pamidronate disodium for injection), another product of Novartis, which is currently used to treat tumor-induced hypercalcemia. The combined results showed that serum calcium levels returned to normal in a statistically significant higher percentage of patients receiving 4 mg Zometa (88.4%) versus those who received Aredia (70%). Moreover, Zometa was infused over 5 minutes, compared to the 2 or more hours required to infuse Aredia. (Zometa is 100-850 times more potent than Aredia.) Responses to Zometa are maintained for long durations (32-39 days). Novartis plans to present an abstract of the clinical trial data at the American Society of Clinical Oncology annual meeting this coming May.

Studies are also under way to assess Zometa for the treatment of bone metastases in patients with solid tumors (including breast, prostate, and lung cancers) and multiple myeloma. Trials to evaluate Zometa for the prevention of bone metastases in prostate cancer have already begun, and similar studies in breast cancer are about to start. Additional studies are planned to explore the potential antitumor effect of Zometa.

What the Patient Should Know

The most common adverse events reported by patients receiving Zometa were bone pain, anemia, fever, nausea, upper respiratory tract infections, fatigue, and constipation – an effects profile similar to that of Aredia.

Brand Name Drug: Innohep
Active Ingredient Drug: tinzaparin sodium
Indication: Treatment of deep vein thrombosis with or without pulmonary embolism when administered in conjunction with warfarin sodium
Company Name: DuPont Pharmaceuticals Company
Availability: Approved by FDA on July 14, 2000

Introduction

Blood clots in the veins, especially in the legs, are a common and very serious problem that affects some 5 million Americans each year. Such deep vein thrombosis (DVT) can lead to pulmonary embolism (a blood clot that travels to the lungs), which develops in about 500,000 people each year and is fatal in some 50,000 of them. DVT accounts for nearly 800,000 hospitalizations each year.

Physicians treating patients with deep vein thrombosis now have another drug in their arsenal, one that can be given only once a day: Innohep (tinzaparin). The drug, a “low-molecular-weight” heparin manufactured by DuPont Pharmaceuticals Company, was approved by the FDA on July 14, 2000 for the treatment of DVT with or without pulmonary embolism when given with warfarin sodium, another anticlotting drug.

Innohep: Clinical Study Results

In once clinical trial, Innohep was compared to unfractionated (conventional) heparin, the most commonly used anticlotting drug, in 435 hospitalized patients with deep vein thrombosis. Innohep was just as effective as standard heparin therapy in the prevention of recurrent DVT and pulmonary embolism. The death rate among patients who received Innohep was 4.6% (10 patients), compared to 9.6% with heparin (21 patients).

Simonneau and colleagues studied 612 patients with pulmonary embolism who received either Innohep or unfractionated heparin. Innohep was found to be equivalent in effectiveness as conventional heparin in these patients, and the risk of major bleeding (a potential side effect of treatment) was similar between the two patient groups.

What You Should Know

The most common side effect in controlled clinical trials evaluating Innohep for deep vein thrombosis treatment was bleeding; however, the incidence of major bleeding was low (0.8% of 519 patients treated with Innohep compared to 2.7% of 524 patients treated with conventional heparin). Like other anticlotting drugs, Innohep should be used with caution in patients with an increased risk of bleeding.

Brand Name Drug: Optivar
Active Ingredient Drug: azelastine hydrochloride
Indication: Treatment of itching of the eye associated with allergic conjunctivitis in adults and children over age 3
Company Name: ASTA Medica
Availability: Approved by FDA on May 22, 2000

Introduction

There’s a new prescription eyedrop available for the millions of Americans who suffer from itchy eyes during hayfever season: Optivar (azelastine hydrochloride ophthalmic solution). The FDA approved the drug — which is manufactured by ASTA Medica — on May 22, 2000. The recommended dosage of the drug is one drop in each affected eye twice daily. Optivar has a rapid onset (within 3 minutes) and a duration of effect of approximately 8 hours for the prevention of itching.

Azelastine is an antihistamine that is also available in nasal spray form, marketed under the brand name Astelin by Wallace Laboratories for the treatment of allergic rhinitis.

How It Works

Optivar is a relatively selective histamine H1 antagonist and an inhibitor of the release of histamine and other mediators from cells involved in the allergic response, including mast cells. Based on in vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (such as leukotrienes and PAF) has been demonstrated with Optivar. Decreased chemotaxis and activation of eosinophils has also been demonstrated.

Optivar (azelastine hydrochloride): Clinical Study Results

Clinical trials have established the efficacy of Optivar (azelastine hydrochloride) for treating allergic conjunctivitis in both adult and pediatric patients. In one randomized, multicenter study, Optivar was compared with placebo and levocabastine eye drops during a 14-day treatment period in 113 children (aged 4 to 12 years) suffering from seasonal allergic conjunctivitis or rhinoconjunctivitis. The primary variable was the response rate, defined as the number of patients showing an improvement after 3 days of treatment in at least 3 score points (from a minimum baseline score of 6) in the main ocular symptoms of itching, conjunctival redness, and lacrimation (each assessed on a 4-point scale). The mean response rate in the Optivar group (74%) was significantly higher than that in the placebo group (39%) and was comparable with that in the levocabastine group. Significant differences for Optivar compared with placebo were observed on days 3 and 14 in the mean sum scores for the three main symptoms and for a total of eight eye symptoms.

Another study assessed the efficacy of 0.025% and 0.05% Optivar in patients with seasonal allergic conjunctivitis of at least a year’s duration. A total of 151 patients received 0.025% or 0.05% Optivar or placebo twice daily for 14 days according to a double-blind, randomized, placebo-controlled, parallel-dosing design; 129 patients completed the study as planned. The three target symptoms, scored on 4-point scales, were itching, lacrimation, and redness of the eyes; responders were patients whose symptom sum score decreased by 3 or more points from a baseline score of at least 6 by day 3. Responder rates were 73% for 0.025% Optivar, 82% for 0.05% Optivar, and 56% for placebo. The time courses of the mean (investigators’ and patients’) scores for the three main symptoms reflected the dose-dependent effect of azelastine eye-drops.

A third double-blind, randomized, placebo-controlled study was performed to assess the efficacy and safety of 0.025% and 0.05% Optivar administered twice daily for 14 days to patients with seasonal allergic conjunctivitis or rhinoconjunctivitis. A total of 278 patients were recruited, and 226 patients were evaluable for analysis. The response rates for itching (improvement of at least one score point within the first three days) according to patient assessment were 43% for placebo, 52% for 0.025% Optivar, and 56% for 0.05% Optivar. However, a more objective assessment of the three main eye symptoms by physicians showed a concentration-dependent improvement in response rate compared with placebo (a decrease of at least 3 points from a baseline total score of at least 6), which reached statistical significance for 0.05% Optivar on day 7. In the evaluable patient population, the scores of the three main eye symptoms as well as of all eight recorded eye symptoms, as assessed by the physician, were significantly lower in the 0.05% Optivar group compared to the placebo group at day 7.

What the Patient Should Know

The most common adverse events reported by patients using Optivar were transient eye burning/stinging, headaches, and bitter taste, all of which were generally mild.

Optivar (azelastine hydrochloride) should not be used to treat irritation related to contact lens wear. Benzalkonium chloride, the preservative in Optivar, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and whose eyes are not red should be instructed to wait at least 10 minutes after instilling Optivar before inserting their contact lenses. Patients should be advised not to wear contact lenses if their eyes are red.

To prevent contaminating the dropper tip and solution, care should be taken not to touch any surface, the eyelids, or surrounding areas with the dropper tip of the bottle.