Spironolactone Hair Loss Treatment-How does it work?
What is Spironolactone?
This is a potassium-sparing diuretic (water pill) that prevents your body from absorbing too much salt and keeps your potassium levels from getting too low. Spironolactone is used in the diagnosis or treatment of conditions in which you have too much aldosterone in your body. Aldosterone is the hormone that is produced by your adrenal glands to help regulate the salt and water balance in your body.
Spironolactone on the other hand also treats fluid retention commonly called edema in people with congestive heart failure, cirrhosis of the liver, or a kidney disorder called nephrotic syndrome. This medication is also used to treat or at times prevent hypokalemia which is a condition characterized by low potassium levels in the blood.
Oral spironolactone is indicated for various conditions and in 1957, it was mainly discovered and used as an antagonist of aldosterone. In this regard, it was used initially as a potassium-sparing diuretic in the treatment of hypertension and congestive heart failure.
Spironolactone is marketed under so many brand names and mostly, it is sold as Aldactone among others. As a medication, it is used to treat fluid buildup as a result of heart failure, liver scarring or kidney diseases. Other indications include blood pressure, low blood potassium, early puberty, and excessive hair growth especially in women. It is also used during the hormone replacement therapy for transgender women. The mode of administration is by mouth.
In most cases, spironolactone is used to treat heart failure, edematous conditions such as nephrotic syndrome or ascites majorly in people with liver disease, essential hypertension, hypokalemia, secondary hyperaldosteronism (such as occurs with hepatic cirrhosis), and Cohn’s syndrome (primary hyperaldosteronism).
On its own, spironolactone is only a weak diuretic because it primarily targets the distal nephron (collecting tubule), where only small amounts of sodium are reabsorbed, but it can be combined with other diuretics to increase efficacy.
What is made up of?
The building block of this drug, is a basic steroidal nucleus with four rings. The primary metabolite of spironolactone is canrenone, which is an active metabolite that is also an antagonist of aldosterone, and thus promotes diuresis.
How does it work for hair?
Technically, spironolactone was found to have antiandrogenic effects when it was first discovered and it was used to treat hypertension in women with concurrent polycystic ovary syndrome (PCOS) and hirsutism.
It antagonizes the androgen receptor as well as inhibiting androgen production. Because of the antiandrogenic effects that result from these actions, it is frequently used off-label to treat a variety of dermatological conditions in which androgens, such as testosterone and dihydrotestosterone are key.
Some of these uses include androgenic alopecia in men (either at low doses or as a topical formulations) and women. It is used to cure hirsutism, acne and seborrheain in women.
Spironolactone is the first line drug used in the treatment of hirsutism. Higher doses of spironolactone are not recommended in males due to the high risk of feminization among other side effects. Similarly, it is also commonly used to treat symptoms of hyperandrogenism in polycystic ovary syndrome.
Spironolactone Male & Female Hair Loss Dosage
Female hair loss Treatment
Androgen receptor blocking drugs such as spironolactone (Aldactone) and finasteride (Propecia) do not approval of FDA for the treatment of female pattern hair loss, and little reliable evidence is available to show that that they are effective.
However, there are some case studies which suggest that women who don’t respond to minoxidil may benefit from the addition of spironolactone. It is in relatively rare cases where there is an excess of androgen, and a clinician may prescribe 100 to 200 milligrams of an androgen receptor blocking drug daily, together with an oral contraceptive for women of reproductive age.
Hair loss male
This drug is mainly used for women. There is no formal approval by the FDA but it is often used by clinicians around the world for 3 primary ‘off use’ uses which are
- Treatment of acne in women
- Treatment of female pattern hair loss (genetic hair loss in women)
- Treatment of hirsutism in women.
The drug blocks the ability of your body to produce testosterone and also blocks the hormone’s receptors in the body. It causes low testosterone in men and hypogonadism.
In men on the other hand, side effects may include loss of male body hair, increased breast development (gynecomastia), impotence and loss of spontaneous erections.
All in all, the drug belongs to a group of drugs that can cause ‘feminization’ in men. You should note that spironolactone is not advised for men with hair loss or acne.
Reviews & Before and After Results
Spironolactone Weight Loss, Gain, Acne
Does the medication Cause;
Cause Weight Loss
It helps in weight loss through an estrogen pathway. Estrogen is an important factor in weight loss. There are several explanations that can be offered to this. The first is that it decreases the activity of fat-absorption within a cell.
The mechanism with which this happens is by decreasing the activity of lipoprotein lipase (LPL). LPL is an enzyme which favors fat uptake into the cells, so having estrogen around inside of a cell helps prevent it from growing larger.
Apart from that, estrogen increases the activity of the enzyme hormone sensitive lipase (HSL). HSL is another major player in regulating a woman’s fat metabolism. Epinephrine stimulates HSL, and then HSL incites lipolysis, and weight loss as a result. HSL activity occurs most commonly in exercise.
There are reports that estrogen is able to stimulate the production of growth hormone. Growth hormone inhibits the uptake of glucose (carbohydrate) by fat tissues and increases the mobilization of fatty acids from fat cells.
The mechanism of action of growth hormone is by inhibiting insulin production from the pancreas and stimulating HSL, which is fat-burning enzyme. Insulin is the main hormone that promotes glucose transport into muscle cells to be used as energy, and it is a potent inhibitor of HSL. For this reason, decreasing insulin levels via GH via estrogen helps speed HSL fat burning activity.
First, fat cells beget estrogen production. But then elevated estrogen levels further slow down metabolism, such that estrogen plays a role in making body to store more weight. For many, this becomes a vicious cycle of accelerating weight gain. The mechanism by which estrogen causes weight gain is through inhibiting thyroid function. In a normal-weight women, estrogen and thyroid hormone play off of each other in an intricate balance.
Yet when a woman becomes overweight, her estrogen levels drive her thyroid function relentlessly downward. With impaired thyroid function, a woman can feel sluggish and fatigued, and therefore expend less energy, and also subconsciously down-regulate her metabolism such that her body is burning less and less fuel to get by and she is not even aware of it.
The aromatase enzymes are available in all types of tissues. Seemingly, the aromatase expressed in adipose tissue accounts for the vast majority of non-ovarian estrogen production in men and in women. This is why, many women suffer estrogen-deficiency symptoms when they lose too much weight.
Similarly, estrogen causes an increase in the receptor anti-lipolytic alpha 2A-adrenergic receptor. This explains how subcutaneous cells maintain their fat mass while other cells do not. In activating this receptor, estrogen increases the number of anti-fat breakdown receptors in subcutaneous fat. Because of the increase in these receptors, cells break down fat less often.
Acne or does it help do away with acne?
Due to spironolactone’s anti-androgen effects, it can be quite effective in clearing severe acne conditions like cystic acne, which is caused by slightly elevated or elevated levels of testosterone in women.
In reducing the levels of testosterone, excess oil that is naturally produced in the skin is also reduced. Though not the primary intended purpose of the medication, its ability to be helpful with problematic skin and acne conditions was discovered to be one of the beneficial side effects and has been quite successful for some time now.
More often, for women treating acne, spironolactone is prescribed and paired with a birth control pill. A significant number of patients have reported that they have seen positive results in the pairing of these two medications, although these results may not be seen for up to three months.
Spironolactone has been used frequently in the dermatology clinic for women with hormonal-pattern AV, defined clinically as primarily inflammatory papules. Many are deep-seated and tender in that they are located predominantly on the lower half of the face and anterior-lateral neck region.
Increased size of sebaceous glands and increased sebum secretion are key components in the development of AV lesions, inhibition of sebaceous gland functions leads to reduced formation of acne lesions. Several studies have shown that spironolactone decreases androgen-stimulated sebocyte proliferation in vitro and inhibits sebaceous activity.
In addition, studies have also shown that acne-prone skin has greater activity of type-1 5-alpha-reductase activity, and non-acne-prone skin has greater activity of 17-beta-hydroxysteroid dehydrogenase activity.
Spironolactone decreases 5-alpha reductase activity via increased clearance of testosterone secondary to augmented liver hydroxylase activity. In addition, it increases the level of steroid hormone binding globulin (SHBG), thus providing a sink that reduces circulating free testosterone as more is bound by the increased quantity of SHBG.
The resultant effect of reducing free testosterone in circulation is an increased estrogenic state, which can lead to gynecomastia or decreased libido, especially when higher doses of oral spironolactone are used.
Side Effects and Safety
The most common side effect of spironolactone is urinary frequency. Other general side effects include
- Dry skin
In males, it has the capability of causing:
- Breast tenderness
- Physical feminization
- Testicular atrophy
- Reversible infertility
- Sexual dysfunction including loss of libido and erectile dysfunction.
In women it causes:
- Menstrual irregularities
- Breast tenderness and enlargement.
The most important potential side effect of spironolactone is hyperkalemia, which, in severe cases, can be life-threatening. Hyperkalemia in these patients can present as a non -anion-gap metabolic acidosis.
Spironolactone may put patients at a heightened risk for gastrointestinal issues like nausea, vomiting, diarrhea, cramping, and gastritis.
In addition, there has been some evidence suggesting an association between uses of the drug and bleeding from the stomach and duodenum, though a causal relationship between the two has not been established. Also, it has been shown to be immunosuppressive in the treatment of sarcoidosis.
Get emergency medical help if you have any signs of an allergic reaction to spironolactone like hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
You should stop using spironolactone and contact your doctor at once if you have the following signs and symptoms:
- signs of stomach bleeding-bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;
- high potassium-slow heart rate, weak pulse, muscle weakness or limp feeling, tingly feeling;
- low sodium-confusion, slurred speech, hallucinations, severe weakness, loss of coordination, feeling unsteady, seizure (convulsions), fainting, shallow breathing (breathing may stop); or
- symptoms of any electrolyte imbalance-dry mouth, increased thirst, drowsiness, lack of energy, restless feeling, confusion, nausea, vomiting, increased urination, muscle cramps or weakness, fast heart rate, little or no urinating, or feeling like you might pass out.
The common spironolactone side effects may include:
- Mild nausea or vomiting, diarrhea;
- Breast swelling or tenderness;
- Dizziness, headache, mild drowsiness;
- Leg cramps; or
- Impotence, difficulty having an erection.