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Understanding Medroxyprogesterone Acetate

Medroxyprogesterone acetate (MPA) is a synthetic progestin used as a contraceptive and to treat various medical conditions. It works by inhibiting gonadotropin production to prevent ovulation and thinning the endometrium. Common side effects include nausea, headaches, weight gain and irregular bleeding. As with any drug, people should see a medical professional to determine if MPA is appropriate and to be aware of any potential adverse reactions based on individual factors.

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55 views5 pages

Understanding Medroxyprogesterone Acetate

Medroxyprogesterone acetate (MPA) is a synthetic progestin used as a contraceptive and to treat various medical conditions. It works by inhibiting gonadotropin production to prevent ovulation and thinning the endometrium. Common side effects include nausea, headaches, weight gain and irregular bleeding. As with any drug, people should see a medical professional to determine if MPA is appropriate and to be aware of any potential adverse reactions based on individual factors.

Uploaded by

Benses Alvarado
Copyright
© All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd

Written Assignment Unit 3

How Do Drug Works

Withheld for peer assessment

Bachelor of Science in health science, UoPeople

BIOL 1301 Introduction to Biology - AY2021-T5

Dr. Rita Mourya (Instructor)

4th July 2021


HOW DO DRUG WORKS 1

Introduction

For personal reasons, I choose “Medroxyprogesterone acetate” (MPA) as my drug

research. It happens that a few days ago, I bought a birth control injection for my wife, and as we

got this assignment and its instructions, I decided to look deeper into this drug.

Medroxyprogesterone acetate

Medroxyprogesterone acetate (MPA) “is a progestin (synthetic) used as a contraceptive

and in the treatment of secondary amenorrhea, abnormal uterine bleeding, pain from

endometriosis, endometrial and renal carcinomas, paraphilia in males, and GnRH-dependent

precocious puberty,  is a progesterone derivative that is more resistant to metabolism for

improved pharmacokinetic properties” (DrugBank, 2005, para. 1-3).

Chemical structure.

MPA is chemically composed of Carbon (C), Hydrogen (H), and Oxygen (O). Its

chemical formula is “C24H34O4 and weight Average: 386.5244, Monoisotopic: 386.245709576”

(DrugBank, 2005, para. 6).

Structure for Medroxyprogesterone acetate


(Credit: DrugBank, 2005)
HOW DO DRUG WORKS 2

Mechanism of action

“Medroxyprogesterone acetate (MPA) inhibits the production of gonadotropin,

preventing follicular maturation and ovulation, which is responsible for its ability to prevent

pregnancy. This action also thins the endometrium. MPA reduces nuclear estrogen receptors and

DNA synthesis in epithelial cells of the endometrium. MPA can also induce p53 dependant

apoptosis in certain cancer cell lines, and inhibit GABA-A receptors” (DrugBank, 2005, para. 7).

Drug inhibitor.

MPA is a “competitive inhibitor and was found to inhibit CYP2C9 and CYP3A4” (Lee,

1999). MPA oral tablets are indicated to treat “secondary amenorrhea, reduce the incidence of

endometrial hyperplasia in postmenopausal women, and to treat abnormal uterine bleeding due

to hormonal imbalance, not organic pathology. Oral tablets containing MPA and conjugated

estrogens are indicated to prevent postmenopausal osteoporosis and to treat moderate to severe

menopausal symptoms such as vasomotor symptoms, vulvar atrophy, and vaginal atrophy.

Subcutaneous MPA is indicated to prevent pregnancy and manage pain associated with

endometriosis. Intramuscular MPA is indicated to prevent pregnancy, and at higher

concentrations for palliative treatment of endometrial or renal carcinoma” (DrugBank, 2005,

para. 5).

Medroxyprogesterone acetate adverse effects.

Some of the most common adverse effects of MPA are, “Nausea, bloating, headache,

changes in appetite, weight gain, tiredness, swelling, acne, hot flashes, breast tenderness, or

irritation/pain at the injection site may occur. Vaginal bleeding between periods (spotting) or
HOW DO DRUG WORKS 3

missed/irregular periods may occur, especially during the first few months of use, may raise

blood pressure,  increase your risk of breast cancer, and may rarely cause serious (sometimes

fatal) problems from blood clots (HealthLinkBC, n.d, para.13). 

Conclusion

In conclusion, it’s our responsibility to choose that we introduce to our body. As

mentioned in this research, MPA has various side effects, so we should be 100% sure and aware

of what we are doing. In addition, we should remember that not all of us have the same

metabolism, and the adverse effect might be different to all of us. Therefore, if we are not sure

how MPA will affect us, we should visits our local medical professional for advice or for

alternative method, that is, if we are using MPA as a contraceptive medication.


HOW DO DRUG WORKS 4

Reference

DrugBank. (2005, June 13). Medroxyprogesterone acetate.

[Link]

HealthLinkBC. (n.d.). Medroxyprogesterone Acetate. Retrieved July 5, 2021, from

[Link]

Lee, T. C. (1999). Medroxyprogesterone acetate. PubMed.

[Link]

%20and%20dexamethasone%20are%20competitive%20inhibitors%20of%20different

%20human%20steroidogenic%20enzymes,-J%20Clin%20Endocrinol

Rye, C., Wise, R., Jurukovski, V., Desaix, J., Choi, J., & Avissar, Y. (2017a). Introduction to

Biology. OpenStax. [Link]

Rye, C., Wise, R., Jurukovski, V., Desaix, J., Choi, J., & Avissar, Y. (2017b). Introduction to

Biology. OpenStax.

[Link]

Biology_Chapters_1-[Link]

Schreiber, C. A., & Barnhart, K. (2014). Medroxyprogesterone Acetate. ScienceDirect.

[Link]

medroxyprogesterone-acetate

Common questions

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MPA's role as a competitive inhibitor of CYP2C9 and CYP3A4 enzymes can lead to interactions with other medications metabolized by these pathways, potentially affecting the metabolism and efficacy of such drugs. This inhibition can lead to increased plasma levels of medications that are substrates for these enzymes, thus requiring careful monitoring and dosage adjustments .

The inhibition of GABA-A receptors by MPA could alter neuronal excitability, potentially affecting mood and anxiety levels. This might provide therapeutic benefits in contexts like paraphilia in males due to reduced impulsivity. However, the impact on normal GABAergic signaling could lead to side effects in susceptible individuals, such as anxiety or depression, complicating its use as a psychiatric medication .

Medroxyprogesterone Acetate (MPA) inhibits the production of gonadotropin, which in turn prevents follicular maturation and ovulation. This effectively blocks the processes necessary for pregnancy to occur. Additionally, MPA thins the endometrium and reduces nuclear estrogen receptors and DNA synthesis in the endometrial epithelial cells .

For reproductive conditions, MPA is mainly used for contraception and to manage issues like amenorrhea and abnormal uterine bleeding. In non-reproductive contexts, it is used for treating conditions such as endometriosis-related pain, and as part of the therapeutic approach for certain carcinomas. Its versatility is due to its hormonal activity and ability to manage estrogen's effects on various tissues .

Medroxyprogesterone Acetate can induce p53-dependent apoptosis in certain cancer cell lines, which is a process where cancerous cells are signaled to die, effectively reducing the size or spread of tumors. It also plays a role in reducing the estrogen receptor activity in these cells, potentially slowing down the progression of the cancer .

MPA is administered in oral tablets, subcutaneous forms, and intramuscular injections. Oral tablets are used to treat secondary amenorrhea, reduce endometrial hyperplasia, and manage menopausal symptoms. Subcutaneous forms prevent pregnancy and manage endometriosis pain. Intramuscular injections are used for contraception and at higher doses for treating endometrial or renal carcinomas .

When prescribing MPA, ethical considerations include ensuring informed consent, where patients are made fully aware of the potential side effects and risks. Physicians should consider the patient's health status, potential interactions with other medications, and individual metabolic profiles. Alternative treatments should be discussed, particularly if the patient has a higher risk of serious adverse effects .

MPA is more resistant to metabolism due to its being a synthetic progestin, which enhances its pharmacokinetic properties. This resistance allows MPA to maintain its effectiveness in inhibiting gonadotropin and preventing follicular maturation and ovulation for an extended period, making it an effective contraceptive .

Common adverse effects of MPA include nausea, bloating, headache, changes in appetite, weight gain, tiredness, and skin issues such as acne. More serious risks include increased blood pressure, elevated risk of breast cancer, and severe blood clotting conditions which can be fatal .

Individual metabolic differences can significantly affect how MPA is processed, leading to variability in the severity and presence of side effects. Some users might metabolize MPA faster, experiencing reduced effects or increased side effects. Others might process it more slowly, which could increase the risk and intensity of adverse effects like blood clot formation or hormonal imbalances .

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