Vegah 100mg by Combitic

Vegah 100mg by Combitic

Product Description
Brand Name:
Vega / Vegah

Generic Name:
Sildenafil Sitrate (generic Viagra)

Sildenafil citrate, sold as Viagra, Revatio and under various other trade names, is a drug used to treat erectile dysfunction and pulmonary arterial hypertension (PAH). It was originally developed by British scientists and then brought to market by the US-based pharmaceutical company Pfizer. It acts by inhibiting cGMP-specific phosphodiesterase type 5 (PDE5), an enzyme that promotes degradation of cGMP, which regulates blood flow in the penis. Since becoming available in 1998, sildenafil has been the prime treatment for erectile dysfunction; its primary competitors on the market are tadalafil (Cialis) and vardenafil (Levitra).

Medical uses:
Sexual dysfunction:
The primary indication of sildenafil is treatment of erectile dysfunction (inability to sustain a satisfactory erection to complete intercourse). Its use is now standard treatment for erectile dysfunction in all settings, including diabetes.

People on antidepressants may experience sexual dysfunction, either as a result of their illness or as a result of their treatment. A 2003 study showed that sildenafil improved sexual function in men in this situation.Following up reports from 1999, the same researchers found that sildenafil improved sexual function in female patients on antidepressants as well.

Pulmonary hypertension:
As well as erectile dysfunction, sildenafil citrate is also effective in the rare disease pulmonary arterial hypertension (PAH). It relaxes the arterial wall, leading to decreased pulmonary arterial resistance and pressure. This, in turn, reduces the workload of the right ventricle of the heart and improves symptoms of right-sided heart failure. Because PDE5 is primarily distributed within the arterial wall smooth muscle of the lungs and penis, sildenafil acts selectively in both these areas without inducing vasodilation in other areas of the body. Pfizer submitted an additional registration for sildenafil to the United States Food and Drug Administration (FDA), and sildenafil was approved for this indication in June 2005. The preparation is named Revatio, to avoid confusion with Viagra, and the 20 milligram tablets are white and round. Sildenafil joins bosentan and prostacyclin-based therapies for this condition.

Altitude sickness:
Sildenafil has been shown to be useful for the prevention and treatment of high-altitude pulmonary edema associated with altitude sickness such as that suffered by mountain climbers.While this effect has only recently been discovered, sildenafil is already becoming an accepted treatment for this condition, in particular in situations where the standard treatment of rapid descent has been delayed for some reason.

Dosage:
Viagra pills are blue and diamond-shaped with the word "Pfizer" engraved on one side, and "VGR xx" (where xx stands for "25", "50" or "100", the dose of that pill in milligrams) engraved on the other. It is taken not more than once per day between 30 minutes and 4 hours prior to sexual intercourse.
The dosage for pulmonary arterial hypertension (Revatio) is three times a day. Revatio pills are white, round, film-coated tablets imprinted with "RVT 20" embossed on one side.

Adverse effects:
In clinical trials, the most common adverse effects of sildenafil use included headache, flushing, dyspepsia, nasal congestion and impaired vision, including photophobia and blurred vision. Some sildenafil users have complained of seeing everything tinted blue (cyanopsia). Some complained of blurriness and loss of peripheral vision. In July 2005, the FDA found that sildenafil could lead to vision impairment in rare cases and a number of studies have linked sildenafil use with nonarteritic anterior ischemic optic neuropathy.

Rare but serious adverse effects found through postmarketing surveillance include priapism, severe hypotension, myocardial infarction (heart attack), ventricular arrhythmias, stroke, increased intraocular pressure, and sudden hearing loss. As a result of these postmarketing reports, in October 2007, the FDA announced that the labeling for all PDE5 inhibitors, including sildenafil, required a more prominent warning of the potential risk of sudden hearing loss.

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Valium 10mg/2ml by Roche

Valium 10mg/2ml by Roche

Product Description
Diazepam Injection:
Each mL of this sterile injection contains 5 mg diazepam compounded with 40% propylene glycol, 10% alcohol, 5% sodium benzoate and benzoic acid as buffers, and 1.5% benzyl alcohol as preservative.

Diazepam is a benzodiazepine derivative. Chemically, diazepam is 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one. It is a colorless crystalline compound, insoluble in water and has a molecular weight of 284.74. The solution is clear, colorless to slightly yellow.

 Diazepam Injection - Clinical Pharmacology:

In animals, diazepam appears to act on parts of the limbic system, the thalamus and hypothalamus, and induces calming effects. Diazepam, unlike chlorpromazine and reserpine, has no demonstrable peripheral autonomic blocking action, nor does it produce extrapyramidal side effects; however, animals treated with diazepam do have a transient ataxia at higher doses. Diazepam was found to have transient cardiovascular depressor effects in dogs. Long-term experiments in rats revealed no disturbances of endocrine function. Injections into animals have produced localized irritation of tissue surrounding injection sites and some thickening of veins after intravenous use.

Usage in Pregnancy:
An increased risk of congenital malformations associated with the use of minor tranquilizers (diazepam, meprobamate, and chlordiazepoxide) during the first trimester of pregnancy has been suggested in several studies. Because use of these drugs is rarely a matter of urgency, their use during this period should almost always be avoided. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered. Patients should be advised that if they become pregnant during therapy or intend to become pregnant they should communicate with their physicians about the desirability of discontinuing the drug.

In humans, measurable amounts of diazepam were found in maternal and cord blood, indicating placental transfer of the drug. Until additional information is available, Diazepam Injection is not recommended for obstetrical use.

Use in Children:

Efficacy and safety of parenteral diazepam has not been established in the neonate (30 days or less of age).

Prolonged central nervous system depression has been observed in neonates, apparently due to inability to biotransform diazepam into inactive metabolites.

In pediatric use, in order to obtain maximal clinical effect with the minimum amount of drug and thus to reduce the risk of hazardous side effects, such as apnea or prolonged periods of somnolence, it is recommended that the drug be given slowly over a three-minute period in a dosage not to exceed 0.25 mg/kg. After an interval of 15 to 30 minutes the initial dosage can be safely repeated. If, however, relief of symptoms is not obtained after a third administration, adjunctive therapy appropriate to the condition being treated is recommended.

Withdrawal symptoms of the barbiturate type have occurred after the discontinuation of benzodiazepines (see DRUG ABUSE AND DEPENDENCE section).

 Precautions:
Although seizures may be brought under control promptly, a significant proportion of patients experience a return to seizure activity, presumably due to the short-lived effect of diazepam after IV administration. The physician should be prepared to readminister the drug. However, diazepam is not recommended for maintenance, and once seizures are brought under control, consideration should be given to the administration of agents useful in longer term control of seizures.

If diazepam is to be combined with other psychotropic agents or anticonvulsant drugs, careful consideration should be given to the pharmacology of the agents to be employed, particularly with known compounds which may potentiate the action of diazepam, such as phenothiazines, narcotics, barbiturates, MAO inhibitors, and other antidepressants. In highly anxious patients with evidence of accompanying depression, particularly those who may have suicidal tendencies, protective measures may be necessary. The usual precautions in treating patients with impaired hepatic function should be observed. Metabolites of diazepam are excreted by the kidney; to avoid their excess accumulation, caution should be exercised in the administration to patients with compromised kidney function.

Since an increase in cough reflex and laryngospasm may occur with peroral endoscopic procedures, the use of a topical anesthetic agent, and the availability of necessary countermeasures are recommended.

Until additional information is available, Diazepam Injection is not recommended for obstetrical use.

Diazepam injection has produced hypotension or muscular weakness in some patients particularly when used with narcotics, barbiturates, or alcohol.

Lower doses (usually 2 mg to 5 mg) should be used for elderly and debilitated patients.

The clearance of diazepam and certain other benzodiazepines can be delayed in association with Tagamet® (cimetidine) administration. The clinical significance of this is unclear.

 Adverse Reactions:
Side effects most commonly reported were drowsiness, fatigue, and ataxia; venous thrombosis and phlebitis at the site of injection. Other adverse reactions less frequently reported include:

Central Nervous System: Confusion, depression, dysarthria, headache, hypoactivity, slurred speech, syncope, tremor, vertigo.

Gastrointestinal: Constipation, nausea.

Genitourinary: Incontinence, changes in libido, urinary retention.

Cardiovascular: Bradycardia, cardiovascular collapse, hypotension.

EENT: Blurred vision, diplopia, nystagmus.

Skin: Urticaria, skin rash.

Other:

Hiccups, changes in salivation, neutropenia, jaundice. Paradoxical reactions such as acute hyperexcited states, anxiety, hallucinations, increased muscle spasticity, insomnia, rage, sleep disturbances and stimulation have been reported; should these occur, use of the drug should be discontinued. Minor changes in EEG patterns, usually low-voltage fast activity, have been observed in patients during and after diazepam therapy and are of no known significance.

In peroral endoscopic procedures, coughing, depressed respiration, dyspnea, hyperventilation, laryngospasm, and pain in throat or chest have been reported.

Because of isolated reports of neutropenia and jaundice, periodic blood counts and liver function tests are advisable during long-term therapy.

Drug Abuse and Dependence:
Diazepam Injection is classified by the Drug Enforcement Administration as a schedule IV controlled substance.

Withdrawal symptoms, similar in character to those noted with barbiturates and alcohol (e.g., convulsions, tremor, abdominal and muscle cramps, vomiting and sweating), have occurred following abrupt discontinuance of diazepam. The more severe withdrawal symptoms have usually been limited to those patients who received excessive doses over an extended period of time. Generally milder withdrawal symptoms (e.g., dysphoria and insomnia) have been reported following abrupt discontinuance of benzodiazepines taken continuously at therapeutic levels for several months. Consequently, after extended therapy, abrupt discontinuation should generally be avoided and a gradual dosage tapering schedule followed. Addiction-prone individuals (such as drug addicts or alcoholics) should be under careful surveillance when receiving diazepam or other psychotropic agents because of the predisposition of such patients to habituation and dependence.



Diazepam Injection Dosage and Administration:
Dosage should be individualized for maximum beneficial effect. The usual recommended dose in older children and adults ranges from 2 mg to 20 mg IM or IV, depending on the indication and its severity. In some conditions, e.g., tetanus, larger doses may be required. (See dosage for specific indications.) In acute conditions the injection may be repeated within one hour although an interval of 3 to 4 hours is usually satisfactory. Lower doses (usually 2 mg to 5 mg) and slow increase in dosage should be used for elderly or debilitated patients and when other sedative drugs are administered. (See WARNINGS and ADVERSE REACTIONS.)

For dosage in infants above the age of 30 days and children, see the specific indications below. When intravenous use is indicated, facilities for respiratory assistance should be readily available.

Intramuscular: Diazepam Injection should be injected deeply into the muscle.

Intravenous Use:

(See WARNINGS, particularly for use in children.) The solution should be injected slowly, taking at least one minute for each 5 mg (1 mL) given. Do not use small veins, such as those on the dorsum of the hand or wrist. Extreme care should be taken to avoid intra-arterial administration or extravasation.

Do not mix or dilute diazepam with other solutions or drugs in syringe or infusion flask. If it is not feasible to administer diazepam directly IV, it may be injected slowly through the infusion tubing as close as possible to the vein insertion.

Once the acute symptomatology has been properly controlled with diazepam injection, the patient may be placed on oral therapy with diazepam if further treatment is required.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

This medication belongs to a class of drugs called benzodiazepines, which act on the brain and nerves (central nervous system) to produce a calming effect. It works by enhancing the effects of a certain natural chemical in the body (GABA) that causes calm.

How to use Valium inj:

This medication is given by injection into a vein or deep into a muscle as directed by your doctor. Giving the medication too fast can cause heart problems. If giving this medication into a vein, inject it slowly into a large vein because the medication is very irritating to the vein. Do not inject this medication into an artery or into the skin.

This medication may be available in a vial, ampule, pre-filled syringe, or pre-filled syringe with autoinjector. The autoinjector automatically delivers a dose of 10 milligrams deep into the muscle. It cannot be used when a lower dose is needed. Do not use the autoinjector for injecting into a vein.

Dosage is based on your medical condition and response to treatment. You will be closely monitored for several hours after receiving this medication. If your doctor orders you to continue to receive this medication, you should be switched to a form that can be taken by mouth as soon as possible.

If you are giving this medication to yourself at home, learn all preparation and usage instructions from your health care professional. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Learn how to store and discard medical supplies safely.

This medication may cause withdrawal reactions, especially if it has been used regularly for a long time or in high doses. In such cases, withdrawal symptoms (such as shakiness, trouble sleeping, muscle cramps, vomiting, sweating, seizures, mental/mood changes such as anxiety/agitation) may occur if you suddenly stop using this medication. To prevent withdrawal reactions, your doctor may reduce your dose gradually. Consult your doctor or pharmacist for more details, and report any withdrawal reactions immediately.

Rarely, abnormal drug-seeking behavior (addiction) is possible with this medication. Do not increase your dose, take it more frequently, or take it for a longer time than prescribed. Properly stop the medication when so directed.

When used for an extended time, this medication may not work as well and may require different dosing. Talk with your doctor if this medication stops working well.

Warnings:
When used intravenously, the following procedures should be undertaken to reduce the possibility of venous thrombosis, phlebitis, local irritation, swelling, and, rarely, vascular impairment; the solution should be injected slowly, taking at least one minute for each 5 mg (1 mL) given; do not use small veins, such as those on the dorsum of the hand or wrist; extreme care should be taken to avoid intra-arterial administration or extravasation.

Do not mix or dilute Diazepam Injection with other solutions or drugs in syringe or infusion flask. If it is not feasible to administer diazepam directly IV, it may be injected slowly through the infusion tubing as close as possible to the vein insertion.

Extreme care must be used in administering Diazepam Injection, particularly by the IV route, to the elderly, to very ill patients, and to those with limited pulmonary reserve because of the possibility that apnea and/or cardiac arrest may occur. Concomitant use of barbiturates, alcohol or other central nervous system depressants increases depression with increased risk of apnea. Resuscitative equipment including that necessary to support respiration should be readily available.

When diazepam is used with a narcotic analgesic, the dosage of the narcotic should be reduced by at least one-third and administered in small increments. In some cases the use of a narcotic may not be necessary.

Diazepam Injection should not be administered to patients in shock, coma, or in acute alcoholic intoxication with depression of vital signs. As is true of most CNS-acting drugs, patients receiving diazepam should be cautioned against engaging in hazardous occupations requiring complete mental alertness, such as operating machinery or driving a motor vehicle.

Tonic status epilepticus has been precipitated in patients treated with IV diazepam for petit mal status or petit mal variant status.

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Klomed 50mg by Ambrosia

Klomed 50mg by Ambrosia

Product Description
Generic Name:
clomiphene citrate

Clomiphene Citrate is typically prescribed for women to aid in ovulation. In men, the application of Clomid causes an elevation of follicle stimulating hormone and luteinizing hormone. As a result, natural testosterone production is also increased.

This effect is obviously beneficial to the athlete, especially at the conclusion of a steroid cycle when endogenous testosterone levels are subnormal. When an athlete discontinues the use of steroids, his testosterone levels will most likely be suppressed. If endogenous testosterone levels are not brought to normal, a dramatic loss in size and strength may occur. Clomid plays a crucial role in preventing this crash in athletic performance.

Bodybuilders find that a daily intake of 50-100 mg of clomiphene citrate over a two week period will bring endogenous testosterone production back to an acceptable level. Clomid will gradually raise testosterone levels over its period of intake. Since an immediate boost in testosterone is often desirable, athlete will commonly use HCG (human choronic gonadotropin) for a couple of weeks, and the continue treatment with Clomid.

Clomid is also effective as an anti-estrogen. Most athletes will suffer from an elevated estrogen level at the conclusion of a cycle. A high estrogen level combined with a low testosterone level puts an athlete in serious risk of developing gynocomastia. With the intake of Clomid, the athlete gets the dual effect of blocking out some of the effects of estrogen, while also increasing endogenous testosterone production.

Package: 10 tabs (50 mg/tab)

Effective Dose: 1 - 2 tabs a day

Clomid (Clomiphene citrate)

Clomid 50 mg. tablets. Each clomid tablet contains 50 mg. clomiphene citrate. Clomid comes in packs of 30 tablets and is manufactured by Effik.

Common uses and directions for Clomid:

Clomid is indicated for the treatment of ovulatory dysfunction in women desiring pregnancy. Impediments to achieving pregnancy must be excluded or adequately treated before beginning Clomid therapy.

The workup and treatment of candidates for Clomid therapy should be supervised by physicians experienced in management of gynecolic or endocrine disorders. Patients should be chosen for therapy with Clomid only after careful diagnostic evaluation.

Treatment of the selected patient should begin with a low dose, 50 mg. daily for 5 days. The dose should be increased only in those patients who do not ovulate in response to cyclic 50 mg. Clomid tablets.

Clomid, at recommended dosages, is generally well tolerated. Adverse reactions are usually mild and transient and most disappear promptly after treatment is discontinued.

Male athletes also find Clomid interesting. In men using Clomid, the elevation in both follicle stimulating hormone and (primarily) luteinizing hormone will cause natural testosterone production to increase. This effect is especially beneficial to the athlete at the conclusion of a steroid cycle when endogenous testosterone levels are depressed. If endogenous testosterone levels are not brought beck to normal, a dramatic loss in size and strength is likely to occur once the anabolics have been removed. Clomid can play a crucial role in preventing this crash in athletic performance.

Clomid (Clomiphene citrate) additional information:

  Common uses:

Clomid tablets, containing clomiphene citrate, is a non steroidal ovulatory stimulant. Clomid is indicated for the treatment of ovulatory dysfunction in women desiring pregnancy. Male athletes also find Clomid interesting. In men using Clomid, the elevation in both follicle stimulating hormone and (primarily) luteinizing hormone will cause natural testosterone production to increase. This effect is especially beneficial to the athlete at the conclusion of a steroid cycle when endogenous testosterone levels are depressed. If endogenous testosterone levels are not brought beck to normal, a dramatic loss in size and strength is likely to occur once the anabolics have been removed. Clomid can play a crucial role in preventing this crash in athletic performance. Directions Clomid comes as a tablet containing 50 mg. clomiphene citrate, to take by mouth. Impediments to achieving pregnancy must be excluded or adequately treated before beginning Clomid therapy. The workup and treatment of candidates for Clomid therapy should be supervised by physicians experienced in management of gynecolic or endocrine disorders. Patients should be chosen for therapy with Clomid only after careful diagnostic evaluation. Treatment of the selected patient should begin with a low dose, 50 mg. daily for 5 days. The dose should be increased only in those patients who do not ovulate in response to cyclic 50 mg. Clomid tablets. For athletes using anabolic steroids, Clomid can normalize the testosterone level and the spermatogenesis (sperm development)within 10-14 days. For this reason Clomid is primarily taken after steroids are discontinued. At this time it is extremely important to bring the testosterone production to a normal level as quickly as possible so that the loss of strength and muscle mass is minimized. 50-100 mg./day seems is a sufficient dosage for athletes. Clomid is usually taken with fluids after meals. If several tablets are taken it is recomended that they be administered in equal doses distributed throughout the day. The duration of Clomid intake should not exceed 10 to 14 days. Most athlets begin with 100 mg./day taking one 50 mg. tablet every morning and evening after meals. After the fifth day the dosage is often reduced to only one 50 mg. tablet per day. If you miss a dose, take it as soon as remembered if it is within an hour or so. If you do not remember until later, skip the missed dose and resume your usual dosing schedule. Do not "double-up" the dose to catch up.
Precautions:

Blurring or other visual symptoms such as spots or flashes may occasionally occur during therapy with Clomid. These visual symptoms increase in incidence with increasing total dose or therapy duration and generally disappear within a few days or weeks after Clomid is discontinued. These visual symptoms may render such activites as driving a car or operating machinery more hazardous than usual, particularly under conditions of variable lighting.
If experiencing visual symptom, treatment should be discontinued and complete ophthalmologic evaluation performed.
There is an increased chance of multiple pregnancy, including bilateral tubal pregnancy and coexisting tubal and intrauterine pregnancy, when conception occurs in relation to Clomid therapy.
It is not known whether Clomid is excreted in human milk. Caution should be exercised if Clomid is administered to a nursing woman. In some individuals, Clomid may reduce lactation.
Prolonged use of Clomid may increase the risk of a borderline or invasive ovarian tumor.

Possible side effects:

Clomid at recommended dosages, is generally well tolerated. Adverse reactions usually have been mild and transient and most have disappeared promptly after treatment has been discontinued. Side effects include ovarian enlargement, vasomotor flushes, abdominal-pelvic discomfort/distention/bloating, nausea and vomiting, breast discomfort, visual symptoms, headache and abnormal uterine bleeding. If you notice other effects not listed above, contact your doctor.

Overdose:

If overdose of Clomid is suspected, contact your local poison control center or emergency room immediately. Toxic effects accompanying acute overdosage of Clomid have not been reported. Signs and symptoms of overdosage as a result of the use of more than the recommended dose during Clomid therapy include nausea, vomiting, vasomotor flushes, visual blurring, spots or flashes, scotomata, ovarian enlargement with pelvic or abdominal pain.

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OC 80mg Generic

OC 80mg Generic

Product Description
OC 80 (Oxycontin 80 mg):
Generic Name:

oxycodone

Pill imprint OC 80 has been identified as Oxycontin 80 mg.

OxyContin is used in the treatment of chronic pain; pain and belongs to the drug class narcotic analgesics. FDA has not classified the drug for risk during pregnancy. OxyContin 80 mg has a high potential for abuse. The drug has a currently accepted medical use in treatment in the United States or a currently accepted medical use with severe restrictions. Abuse of the drug may lead to severe psychological or physical dependence.

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Kinz (Nalbuphine) 10mg by Sami

Kinz (Nalbuphine) 10mg by Sami

Product Description
NUBAIN (nalbuphine hydrochloride):

nubain is  a synthetic agonist-antagonist of the phenanthrene series. It is  chemically related to both the widely used opioid , , and the potent  opioid analgesic, oxymorphone. Chemically nalbuphine hydrochloride is  17-(cyclobutylmethyl)-4,5α-epoxymorphinan-3,6α,14-triol hydrochloride.  Nalbuphine hydrochloride molecular weight is 393.91 and is soluble in H2O (35.5 mg/mL @ 25ºC) and ethanol (0.8%); insoluble in CHCl3 and ether. Nalbuphine hydrochloride has pKa values of 8.71 and 9.96. The molecular formula is C21H27NO4·HCl.  NUBAIN  is a sterile solution suitable for subcutaneous, intramuscular, or  intravenous injection. NUBAIN is available in two concentrations, 10 mg  and 20 mg of nalbuphine hydrochloride per mL. Both strengths in 10 mL  vials contain 0.94% sodium citrate hydrous, 1.26% citric acid anhydrous,  and 0.2% of a 9:1 mixture of methylparaben and propylparaben as  preservatives; pH is adjusted, if necessary, to 3.5 to 3.7 with  hydrochloric acid. The 10 mg/mL strength contains 0.2% sodium chloride. NUBAIN  is also available in ampuls in a sterile, paraben-free formulation in  two concentrations, 10 mg and 20 mg of nalbuphine hydrochloride per mL.  One mL of each strength contains 0.94% sodium citrate hydrous, and 1.26%  citric acid anhydrous; pH is adjusted, if necessary, to 3.5 to 3.7 with  hydrochloric acid. The 10 mg/mL strength contains 0.2% sodium chloride.

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Arimidx 1mg by Astra Zeneca

Arimidx 1mg by Astra Zeneca

Product Description
Anastrozole (INN) (marketed under the trade name Arimidex by AstraZeneca) is an aromatase-inhibiting drug approved for treatment of breast cancer after surgery, as well as for metastasis in both pre and post-menopausal women. The severity of breast cancer is increased by estrogen, as sex hormones cause hyperplasia, and differentiation at estrogen receptor sites. Anastrozole works by inhibiting the synthesis of estrogen
Medical uses:
The ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial was an international randomised controlled trial of 9366 women with localized breast cancer who received either anastrozole, tamoxifen, or both for five years, followed by five years of follow-up. After more than 5 years the group that received anastrozole had significantly better clinical results than the tamoxifen group. The trial suggested that anastrozole is the preferred medical therapy for postmenopausal women with localized breast cancer that is estrogen receptor (ER) positive. Another study found that the risk of recurrence was reduced 40%, which also included an increased risk of bone fractures, and that ER negative patients benefited from switching to anastrozole.

Mechanism of action:
Anastrozole binds reversibly to the aromatase enzyme through competitive inhibition, inhibits the conversion of androgens to estrogens in peripheral tissues (outside the CNS), and a few CNS sites in various regions within the brain.

Side effects:
Bone weakness has been associated with anastrozole. Women who switched to anastrozole after two years on tamoxifen reported twice as many fractures as those who continued to take tamoxifen (2.1% compared to 1%). Bisphosphonates are sometimes prescribed to prevent the osteoporosis induced by aromatase inhibitors. The level of circulating oestradiol is likely causal here and not the anastrozole itself, and so the dose will determine likelihood of osteoporosis (oestradiol inhibits osteoclasts, which resorb bone).

Usage in men:
Anastrozole has been tested for reducing estrogens, including estradiol, in men. Excess estradiol in men can cause benign prostatic hyperplasia, gynecomastia, and symptoms of hypogonadism. It can also contribute to increased risk of stroke, heart attack, chronic inflammation, prostate enlargement and prostate cancer. Some athletes and body builders use anastrozole as part of their steroid cycle to reduce and prevent symptoms of excess estrogen--gynecomastia, emotional lability and water retention. Study data suggests dosages of 0.5 mg to 1 mg a day reduce serum estradiol approx. 50% in men, which differs in postmenopausal women.

Usage in children;
Anastrozole may be used off-label in children with precocious puberty, or children with pubertal gynecomastia. Following the onset of puberty, the epiphyseal plate begins to close due to an increased amount of estrogen production escaping local metabolism and spreading to the circulatory system. It is shown to help slow this process, and increase adult height prediction in adolescent males treated with protein-based peptide hormones for the treatment of growth hormone deficiency

Chemical synthesis:
The synthesis begins with nucleophilic substitution of two benzylic bromides in α,α'-dibromomesitylene (prepared by radical bromination of mesitylene, not shown on the scheme) with cyanide by treatment with potassium cyanide under phase transfer conditions, affording the dinitrile. Exhaustive methylation with methyl iodide and sodium hydride leads to the replacement of the more acidic side chain hydrogen atoms by methyl groups. The treatment with bromine in the presence of benzoyl peroxide leads to the formation of the corresponding benzyl bromide. Reaction of that product with 1,2,4-triazole in the presence of a base completes the synthesis of the aromatase inhibitor.

Important information about Arimidex;
Do not use Arimidex if you are pregnant. It could harm the unborn baby.

You may need to take a pregnancy test before using Arimidex, to make sure you are not pregnant.

You should not use Arimidex if you are allergic to anastrozole, if you are breast-feeding a baby, or if you have not yet completed menopause. Arimidex is not for use in men or children.

Before using Arimidex, tell your doctor if you have heart disease, circulation problems, a history of stroke or blood clot, severe liver disease, high cholesterol, osteoporosis, or low bone mineral density.

Arimidex may not work as well if you take it together with tamoxifen or an estrogen medication (such as hormone replacement therapy, estrogen creams, or birth control pills, injections, implants, skin patches, and vaginal rings). Before you start taking this medicine, tell your doctor if you also take tamoxifen or estrogen.

You may need to keep taking Arimidex for up to 5 years. Follow your doctor's instructions.

Before taking Arimidex:
You should not use Arimidex if you are allergic to anastrozole, if you are breast-feeding a baby, or if you have not yet completed menopause. Arimidex is not for use in men or children.

To make sure you can safely take Arimidex, tell your doctor if you have any of these other conditions:

heart disease;

circulation problems;

a history of stroke or blood clot;

severe liver disease;

high cholesterol; or

osteoporosis or low bone mineral density.

Arimidex can decrease bone mineral density, which may increase your risk of developing osteoporosis. Your bone mineral density may need to be tested before and during treatment with this medicine.

FDA pregnancy category D. Do not use Arimidex if you are pregnant. It could harm the unborn baby. Use effective birth control, and tell your doctor if you become pregnant during treatment. It is not known whether anastrozole passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are using Arimidex.

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