What is Letrozole aka Cabergoline?
Letrozole is used in the treatment of different kinds of male infertility by indirectly increasing their testosterone levels. It is also popular among bodybuilders for increasing muscle strength and boosting testosterone levels. In bodybuilders, it is also utilized in decreasing gynecomastia which occurs while consuming anabolic steroids for muscle mass accumulation.
Letrozole for Bodybuilding
Letrozole works to prevent estrogen production, which in turn increases testosterone productions. Still, confused? Let us make it simpler for you.
In men, a small quantity of free testosterone is converted into estradiol, which is a version of estrogen. With the increase in age, the body of men starts producing less testosterone, and more estradiol. Higher estrogen levels are linked to infertility.
For muscle builders particularly, estrogen levels need to be regulated as, they’re linked to a gain in weight, decreased growth in muscle, man breasts or gynecomastia, and lowered sex drive.
How to use Letrozole
It’s quite easy to use any medicine, so what’s the point of delineating the usage directions of letrozole? Well, the answer is, there is a set of guidelines specific to every drug which need to be followed to get maximum benefits from that medication. The patient guideline pamphlet contains all the essential information required for a patient using letrozole for the first time. You must consult your physician in case of any questions or emergency.
This drug is consumed orally, once a day along with food or without it. It must be consumed as per the directions of your physician. This drug should be used frequently for getting the best positive results. To avoid the hassle of forgetting about the drug consumption each day, as it so happens we recommend crossing out the prescribed days on your calendar to help with the drug uptake regularly.
Mechanism of Action of Letrozole
Letrozole is a potent drug belonging to the class of drugs called aromatase inhibitors. These drugs are used to decrease the conversion of estrogen, as they inhibit the enzyme aromatase, required in a significant step in estrogen hormone production. Letrozole is a nonsteroidal inhibitor of estrogen production with antitumor activity. This action helps in letrozole fertility.
It reversibly and selectively inhibits aromatase. This drug works by obstructing the activity of aromatase, which is used in the conversion of androgens to estrogens in a process known as aromatization, hence the name aromatase. This drug is orally active and is an antiestrogen. This drug prevents the production of estrogen by attaching competitively to aromatase. This mechanism aids in Letrozole bodybuilding.
Optimal Letrozole Dosage
The favorable dose consumption of this drug depends on the medical condition of a person, and the effects for which that medication is being used. The general optimal dosage of this drug is usually one tablet consumed per day. This drug comes in the form of 2.5mg tablets. You should try to take letrozole around the same time every day so that it can work better, and your body’s natural clock can better grow accustomed to it.
You must swallow the whole tablet with a glass of water. You mustn’t try to crush or chew it.
The generic name of this drug is Letrozole, which is generally sold under the brand name of Femara among others.
Interactions with other Medications
This medication has the possibility of interfering or interfacing with other drugs that you are possibly using for other medical conditions. The drug interactions might alter the efficacy of a drug or multiply the serious side effects risk.
Some medications which might interfere with letrozole are, estrogens, like ethinyl estradiol, or conjugated estrogens, estrogen blockers like anastrozole or tamoxifen, and tibolone. Tamoxifen results in blood letrozole levels decline if consumed together. As Letrozole is an anti-estrogen drug, so the estrogen-containing substances result in nullification of the effects of letrozole.
This medication cannot be consumed alongside tamoxifen or ethinylestradiol, both of which work to reduce the effects or levels of letrozole by acting as antagonists. The performance of letrozole needs to be carefully monitored when given with dengue vaccine, letermovir, cholera vaccine, siponimod, or eluxadoline.
Are there any Side Effects of Letrozole?
Yes of course! This medication is no different than any other drug, so its use is also presented by a possibility of various side effects including,
- Extreme sweating
- Loss of hair
- Aches in muscles, bones, and joints
- Fatigue
- Drowsiness
- Nausea
- Digestive problems
- Vertigo
- Problems with sleeping
- Hot flashes
- Extremely high levels of testosterone
You will need to notify your physician if any of these symptoms exacerbate or persist for prolonged periods.
Side effects like severe allergic reaction are rare, however, in case of symptoms like extreme rash, itching, swelling, labored breathing, and drowsiness, you must seek immediate medical attention.
Letrozole Overdosage
You should visit your doctor right away, in case you notice serious side effects like,
- Fractures in bone
- Mode alterations
- Swelled legs and arms
- Blurriness of vision
- Extreme fatigue
- Yellowing of the skin and eyes
- Dark-colored urine
Are There any Storage Guidelines and Precautions?
Yes! This medication needs to be stored in the holder that it came in, must be closed tightly, and kept out of reach of children. It needs to be stored at room temperature, in a cold dry environment, away from excessive sunlight, warm temperatures, and humidity. So if you’re used to storing your medications in your bathroom cabinet, you’ll need to mend your ways for this medicine.
References
- Dellapasqua, S., 2010. Letrozole. Expert Opinion on Drug Metabolism and Toxicology, 6(, pp. 251-259.
- Dowsett, M., 1999. Drug and hormone interactions of aromatase inhibitors.. Endocrine-Related Cancer.
- Peivandi, S., 2019. Effect of letrozole on spermogram parameters and hormonal profile in infertile men A clinical trial study. NCBI.
Other Products That May Interest You
Triazide, Femara, Arimidex, Aromasin
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Common Letrozole Questions
How to take letrozole for fertility?
Using 2.5 mg letrozole pill once a week has proved to be extremely significant in the restoration of infertility in men for a period ranging from 2 to 21 months. These results were shared by a research group working at CHUM, San Diego.
How long does letrozole stay in your system?
In the light of conducted research, it was found that approximately 90% of radio-tagged letrozole is excreted in the urine. Letrozole terminal half-life was found to be 2 days, with normal plasma levels following regular 2.5mg dose being restored in 2-6 weeks.
What happens when you stop taking Letrozole?
Many people fear that discontinuing this drug will be immediately accompanied by withdrawal symptoms; however, you don’t need to worry as this drug has not shown to cause any known withdrawal symptoms.
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