Progesterone
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Progesterone is a steroid hormone produced in ovaries and testes that promotes endometrial development and inhibits ovulation. It works by negatively feedbacking at the hypothalamus to decrease gonadotropin release from the pituitary gland. Synthetic progestogens are used in contraceptives due to their stability. Contraceptives prevent pregnancy through a combination of estrogen suppression of LH and FSH and progestin thickening of cervical mucus. Common contraceptive methods include oral pills, transdermal patches, injections, and implants containing estrogen and progestin combinations. Adverse effects include breast changes, fluid retention, headaches and changes in mood and libido.
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PROGETINS
Progesterone is a hormone that prepares the uterus for pregnancy and maintains pregnancy. It is produced naturally by the ovaries and placenta during pregnancy. Synthetic progestins are also used as contraceptives and for hormone replacement therapy. Progestins work by converting the estrogen-primed endometrium to a secretory state and maintaining it to support pregnancy. They also have other effects throughout the body. Mifepristone is a progesterone antagonist that is used to terminate early pregnancies by blocking the effects of progesterone and causing abortion.
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This document discusses drugs used in reproductive health, including estrogens, progestins, and oral contraceptives. It provides details on:
1) Estrogens like estradiol that are responsible for female pubertal changes and progesterone that prepares the uterus for pregnancy.
2) Oral contraceptives that contain estrogen and progesterone to prevent ovulation and thickening of cervical mucus to inhibit sperm penetration.
3) Different types of combined oral contraceptives including triphasic pills that mimic the hormonal cycle, and progestin-only mini pills.
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This document summarizes key information about estrogens:
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2. It explains the mechanisms of action of estrogens, including their binding to estrogen receptors, dimerization, and gene transcription effects.
3. It outlines the therapeutic uses of estrogens like hormone replacement therapy and the pharmacological actions and regulation of estrogen secretion.
Estrogen and Antiestrogen.pptx
Tamoxifen is used for prophylaxis of breast cancer in high-risk women. It works by competing with estrogen for binding to estrogen receptors in breast tissue, thereby blocking the normal stimulatory effects of estrogen on breast growth. Some breast tumors may regress with tamoxifen treatment due to this antagonism of estrogen receptors in breast cells. The drug is administered orally where it undergoes extensive metabolism by the CYP450 system.
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Progestins
progestins pharmacology and different forms of it............................................................................................................................................................................................................................................
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Progesterone is a hormone that prepares the uterus for pregnancy and maintains pregnancy. It is produced naturally by the ovaries and placenta during pregnancy. Synthetic progestins are also used as contraceptives and for hormone replacement therapy. Progestins work by converting the estrogen-primed endometrium to a secretory state and maintaining it to support pregnancy. They also have other effects throughout the body. Mifepristone is a progesterone antagonist that is used to terminate early pregnancies by blocking the effects of progesterone and causing abortion.
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1) Estrogens like estradiol that are responsible for female pubertal changes and progesterone that prepares the uterus for pregnancy.
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2. It explains the mechanisms of action of estrogens, including their binding to estrogen receptors, dimerization, and gene transcription effects.
3. It outlines the therapeutic uses of estrogens like hormone replacement therapy and the pharmacological actions and regulation of estrogen secretion.
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3. The menstrual cycle consists of the menstrual, proliferative, and secretory phases regulated by fluctuating estrogen and progesterone levels.
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- There are two major progesterone receptor subtypes, PRA and PRB. PRA inhibits the effects of PRB and other steroid receptors in many tissues where they are expressed.
- Micronized natural progesterone from plant sources has fewer side effects than older synthetic progestins and more closely mimics the body's endogenous progesterone. It can be administered orally, vaginally, or through other routes.
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Progesterone is a natural hormone that prepares the uterus for pregnancy and helps maintain pregnancy. It can be produced naturally by the body or synthesized for medical uses. Progesterone has physiological actions in the uterus, cervix, vagina, breasts, central nervous system, and elsewhere to support pregnancy. It works by binding to progesterone receptors and regulating gene transcription. Progesterone and progestins are used for contraception, hormone replacement therapy, dysfunctional uterine bleeding, threatened miscarriage, endometriosis, and other conditions. Common side effects include changes in menstruation, headaches, and breast tenderness.
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Oral contraceptives, also known as birth control pills, come in combined and progestogen-only formulations. Combined pills contain estrogen and progestogen, while progestogen-only pills only contain progestogen. Their main mechanisms of action are to prevent ovulation and make cervical mucus inhospitable to sperm. Potential adverse effects include cardiovascular risks, changes in serum lipids, and metabolic effects. Oral contraceptives have been shown to decrease risks of some cancers while their effects on other cancers are still debated.
24.复件 Family Panning2008
The document discusses various methods of contraception including oral contraceptives, long-acting contraceptive injections, implants, intrauterine devices, and vaginal rings. It provides details on the components, effectiveness, use directions, side effects, and contraindications of different contraceptive methods. The summary focuses on key contraceptive options and their effectiveness rates based on studies.
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2. Progesterone regulates the uterine cycle and maintains pregnancy. It is produced in the corpus luteum, placenta, and adrenal cortex.
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1) Ritoridine is a beta-2 selective adrenergic agonist that can suppress premature labor and delay delivery for up to 48 hours. However, it can cause side effects like hypotension, tachycardia, hyperglycemia, and neonatal issues.
2) Nifedipine is a calcium channel blocker that reduces uterine tone and contractions by acting as a prominent smooth muscle relaxant. It can cause maternal tachycardia and hypotension as well as fetal hypoxia.
3) Atosiban is an oxytocin receptor antagonist that may be available in Nepal, though its availability
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The two main sex hormones — estrogen and testosterone — have wide-ranging effects in the body. Produced primarily by the ovaries (estrogen) and testes (testosterone), these hormones affect not just your sexual function but also your bones, brain, and blood vessels.
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Dydrogesterone is a progestin hormone used to regulate the healthy growth and shedding of the womb lining. It was first introduced in 1961 and is now approved in over 100 countries. It works by selectively binding to progesterone receptors and has an active metabolite called 20α-dihydrodydrogesterone that is non-sedative. Dydrogesterone is used orally at doses of 5-40 mg daily or via intramuscular injection of 100 mg daily to treat menstrual disorders, prevent miscarriage, treat endometriosis, support fertility, and prevent thickening of the uterine lining during hormone replacement therapy. Common side effects include headaches, breast pain or tenderness, spotting, and changes to menstrual periods
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This document discusses hormonal contraceptives, including their mechanisms of action and types. It begins by listing the possible methods of contraception and then focuses on hormonal methods. It explains that hormonal contraceptives work by suppressing GnRH and the subsequent release of LH and FSH from the pituitary gland, preventing follicle maturation and ovulation. The main types discussed are combined oral contraceptive pills containing estrogen and progestin, progestin-only pills, and emergency contraception. Combined pills can be monophasic, biphasic, or triphasic depending on hormone levels. Potential side effects and regimens for emergency contraception are also summarized.
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- Progesterone is a steroid hormone that plays several important roles in the female reproductive system and pregnancy. It can be produced naturally in the body or taken as a synthetic progestin medication.
- There are two major progesterone receptor subtypes, PRA and PRB. PRA inhibits the effects of PRB and other steroid receptors in many tissues where they are expressed.
- Micronized natural progesterone from plant sources has fewer side effects than older synthetic progestins and more closely mimics the body's endogenous progesterone. It can be administered orally, vaginally, or through other routes.
- Progesterone supplementation shows benefits for preventing preterm birth and recurrent pregnancy loss according to some studies,
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Mass spectrometry involves ionizing molecules and separating the resulting ions based on their mass-to-charge ratio. The technique can determine molecular mass and formula. It works by bombarding molecules with electrons to produce radical cations, accelerating the ions in an electric field to separate them based on m/z, and detecting the ions. Isotopic abundances provide additional structural information, such as the number of carbon or halogen atoms present.
Diuretics
The kidneys lie on the posterior abdominal wall, one on each side of the vertebral column, behind the peritoneum and below the diaphragm
The nephron consists of a tubule closed at one end, the other end opening into a collecting tubule
Continuing from the glomerular capsule the remainder of the nephron is about 3 cm long and is described in three parts:
the proximal convoluted tubule
the medullary loop (loop of Henle)
the distal convoluted tubule, leading into a collecting duct
High efficacy diuretics (Inhibitors of Na-+K+-2Cl¯ cotransport)
Sulphamoyl derivatives : Furosemide, Bumetanide, Torasemide
2. Medium efficacy diuretics (Inhibitors of Na+-Cl¯ symport)
Benzothiadiazines (thiazides) Hydrochlorothiazide, Benzthiazide, Hydroflumethiazide, Bendroflumethiazide
Thiazide like (related heterocyclics) Chlorthalidone, Metolazone, Xipamide, Indapamide, Clopamide
3. Weak or adjunctive diuretics
(a) Carbonic anhydrase inhibitors : Acetazolamide
(b) Potassium sparing diuretics
Aldosterone antagonist: Spironolactone, Eplerenone
Inhibitors of renal epithelial Na+ channel: Triamterene, Amiloride.
(c) Osmotic diuretics :Mannitol, Isosorbide, Glycerol
Mass spect. m. pharm
The Mass Spectrometer
Quadrupole Mass Spectrometer
The compact size and speed of the quadrupole instruments lends them to be efficient and powerful detectors for gas chromatography (GC)
Since the compounds are already vaporized, only the carrier gas needs to be eliminated for the process to take place
The interface between the GC and MS is shown; a “roughing” pump is used to evacuate the interface
Role of free radical in neurodegenerative disease
ROLE OF FREE RADICAL IN NEURODEGENERATIVE DISEASE
Oxidative stress in AD??
Oxidative stress occurs when there is an imbalance between t he production and quenching of free radicals from oxygen species. These reactive oxygen species (ROS) play a role in many chronic diseases including mitochondrial diseases, neurodegenerative diseases, renal disease, arteriosclerosis, diabetes , cancer.
The process of aging is also associated with increased oxidative stress. Through pathological redox reactions ROS can denature biomolecules such as proteins, lipids and nucleic acids. This can initiate tissue damage via apoptosis and necrosis.
Oxidative stress plays a central role in the pathogenesis of AD leading to neuronal dysfunction and cell death.
Peripheral markers of oxidative stress are elevated in AD indicating that the damage is not brain-limited.
The increased level of oxidative stress in the AD brain is reflected by
increased protein and DNA oxidation,
Decreased level of cytochrome C oxidase and advanced glycosylation end products.
enhanced lipid peroxidation,
Lipid peroxidation can weaken cell membranes causes ion imbalance and impair metabolism.
Oxidative stress can influence DNA methylation which regulates gene expression.
Internalized beta-amyloid may play a role in this process.
Mitochondrial dysfunction, which is associated with an accumulation of ROS, appears to play a role in the early events of AD pathology.
Generation and role of free radicals 11
Free radicals are unstable, highly reactive molecules which are generated both in the body and outside the body. They are described as electron hungry molecules produced when oxygen is metabolized or burned by the body
Role of Free Radical in diseases
Icmr guidelines
Responsible conduct of research .
• The responsible conduct of research (RCR) involves the following major components: values; policies; planning and conducting research; reviewing and reporting research; and responsible authorship and publication
• Institutions conducting research must establish a research office within their institution to facilitate research, manage grants, and oversee all aspects of RCR
• The research office must work closely with the EC and with all stakeholders, including undergraduate and postgraduate students
• SOPs required to address components of RCR as follows
–Values of research
- RCR is guided by shared values including honesty, accuracy, efficiency, fairness, objectivity, reliability, accountability, transparency, personal integrity, and knowledge of current best practices, and these should be reflected in RCR-related policies
–Policies
- Protection of human participants, animal experimentation
–Planning and conducting research - specific issues
- Conflict of interest; data acquisition, management, sharing and ownership
–Reviewing and reporting research
–Responsible authorship and publication
–Research misconduct and policies for handling misconduct
–Registration with Clinical Trials Registry- India
–Collaborative research
Ethical review procedures
Ethical review procedures
• Terms of reference for ethics committees (EC)
–TOR for the EC and its members should be clearly specified by the institution in the EC SOPs
• Special situations
–Institutions can have one or more than one EC; each EC can function as a stand-alone committee which should follow all the SOPs and TORs of that institution
–An institution that does not have its own EC (user institution) may utilize the services of the EC of another institution (host institution) preferably in the adjoining/nearby area
• List of SOPs
• Review of multicentric research
• Continuing review
• Site monitoring
• Record keeping and archiving
• Administration and management
• Registration and accreditation of ECs
• Criteria for selection of EC members
• Composition of an EC
Schedule y
DETAIL ABOUT PHARMACOVIGILANCE TOPIC SCHEDULE Y.
DEFINITION, DETAIL, RULES AND REGULATIONS
easy to study about it.
clinical trials in schedule.
Salient Features of Schedule Y
Copd drugs
ASTHMA AND COPD FULL DETAIL IN EASY PROCESS,
chronic obstructive pulmonary disease. DEFINATION AND REASONS, FACTORS OF IT, INTRINSIC AND EXTRINSIC FACTORS
Drug discovery finding a lead
Scientists are constantly searching for new drug leads through screening thousands of potential candidate compounds. Once a promising lead compound is identified, medicinal chemists will then modify its structure to improve potency and safety based on structure-activity relationships. The lead optimization process aims to develop a clinical candidate drug with desirable pharmaceutical properties for testing in human clinical trials.
Estrogen
Estrogens are a group of female sex hormones that promote female characteristics. The major estrogens produced by women are estradiol, estrone, and estriol. Estradiol is the major secretory product of the ovaries and is regulated by FSH and LH from the hypothalamus and pituitary gland. Estrogens have various therapeutic uses including relieving menopausal symptoms, contraception, and developing secondary sex characteristics. They are absorbed through the GI tract, skin, and mucous membranes and metabolized in the liver primarily being excreted in urine. Adverse effects include breast tenderness, nausea, and increased cancer risk. Anti-estrogen drugs include competitive receptor inhibitors, aromatase
Calcium regulation
Calcium metabolism and its regulation involves several key processes:
- Calcium exists in the body in hydroxyapatite form and ionized/protein-bound plasma forms. Requirements vary by age.
- Calcium is absorbed in the small intestine through a carrier protein aided by vitamin D, PTH, and acidity. Absorption is regulated by hormones including PTH, calcitonin, and vitamin D.
- Calcium has many biological functions including bone/tooth mineralization and cellular processes. Hormones like PTH and calcitonin tightly regulate calcium levels through effects on bones and kidneys.
Adrenal hormones
The adrenal glands produce three main types of hormones - glucocorticoids, mineralocorticoids, and androgens. The adrenal cortex synthesizes these hormones from cholesterol. Glucocorticoids like cortisol regulate metabolism and stress response. Mineralocorticoids like aldosterone regulate salt and water levels. Adrenal hormones act through intracellular receptors in target tissues. Cortisol increases blood glucose levels while aldosterone increases blood volume by regulating sodium and potassium. These hormones are used clinically to treat conditions like adrenal insufficiency, inflammation, and allergies. Their administration requires consideration of factors like dosage, activity, and duration of action to avoid adverse effects.
Angrogens
Androgens are a group of steroids that have masculinizing effects in both males and females. Testosterone is the most important androgen, produced primarily in the testes in males and in smaller amounts in ovaries and adrenal glands of both sexes. Androgens are required for normal male maturation, sperm production, muscle growth, and bone strength. They work by binding to nuclear receptors in target cells. Therapeutic uses include treatment of hypogonadism and wasting diseases, while adverse effects include acne, hair growth, and prostate issues. Antiandrogens can counter male hormonal actions and are used to treat prostate cancer.
Nsaids
NSAIDs work by inhibiting the cyclooxygenase (COX) enzyme and preventing the synthesis of prostaglandins. This summary inhibition of prostaglandin synthesis is responsible for their analgesic, antipyretic and anti-inflammatory effects. However, it can also lead to unwanted side effects like gastric irritation. NSAIDs can be classified based on their structure and selectivity for the COX-1 or COX-2 isoenzyme. The document discusses the mechanism of action, classification, synthesis and structure-activity relationships of various NSAIDs.
Antiosteoporotic 1
1) The document presents research on the anti-osteoporotic effects of Salvadora persica stick extract (SPE) in an estrogen-deficient rat model of osteoporosis.
2) Methods included administering SPE orally to ovariectomized (OVX) rats at various doses for 16 weeks, and measuring bone mineral density, biomechanical strength, and biochemical markers of bone turnover.
3) Results showed SPE increased bone mineral density and biomechanical strength in a dose-dependent manner, and reduced bone turnover, indicating a protective effect against osteoporosis in OVX rats.
Osteoporosis in detail
The document discusses molecular mechanisms of osteoporosis. It defines osteoporosis as a medical condition where bones become brittle and fragile from loss of tissue, often due to hormonal changes or deficiencies in calcium or vitamin D. The document outlines that bones are composed of an organic matrix and inorganic minerals including calcium, phosphorus, and collagen. It also describes the roles of osteocytes, osteoblasts, and osteoclasts in bone formation and resorption. Pathways involved in osteoporosis pathogenesis include glucocorticoid signaling and molecular signals such as RANKL, DKK-1, and sclerostin. Treatments discussed are antibody therapies targeting these molecules as well as stem cell therapy and
Hyperlipidemia
This document discusses hyperlipidemia, which refers to abnormally high lipid levels in the blood. It defines hyperlipidemia and describes the pathophysiology involving cholesterol transport. The document outlines the diagnosis of hyperlipidemia through lipid profile testing and lists common causes such as diet, obesity, medications, and medical conditions. It also describes the types of hyperlipidemia based on increased lipoproteins, associated symptoms, prevention strategies involving diet and exercise, drug treatment options by class and their mechanisms of action, and potential side effects.
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Progesterone
- 1. Progesterone and contraceptives Presented by- SHOUVIK KUMAR NANDY 1
- 2. Progesterone is a steroid Produced in ovaries by corpus luteum under the influence of luteinising hormone(LH) from anterior pituitary and in males (secreted by the testes) 2
- 3. Ross and Wilson, Anatomy and physiology in health and illness, ninth edition, 3
- 4. Mechanism of action In females, progesterone promotes the development of a secretory endometrium that can accommodate implantation of a newly forming embryo The high levels of progesterone that are released during the second half of the menstrual cycle (the luteal phase) inhibit the production of gonadotropin and, therefore, prevent further ovulation Lippincott illustrated review Pharmacology, Sixth edition, page no.- 355-357 4
- 5. Progesterone negatively feedback works at hypothalamus to decrease the pulse frequency of gonadotropin releasing hormone This in turn will decrease the secretion of follicle stimulating hormone(FSH) and decrease the secretion of luteinizing hormone(LH) Progesterone ability to inhibit sperm from penetrating through the cervix and upper genital track by making the cervical mucus unfriendly 5
- 6. Therapeutic uses of progestogens The major clinical uses of progestogens are for contraception or the treatment of hormone deficiency For contraception, they are often used in combination with estrogens Synthetic progestogens used in contraception are more stable to first pass metabolism These agents include desogestrel, levonorgestrel 6
- 7. Pharmacokinetics A micronized preparation of progesterone is rapidly absorbed after oral administration It has a short half-life in the plasma and is almost completely metabolized by the liver The glucuronidated metabolite is excreted primarily by the kidney 7
- 8. Adverse effect The major adverse effects associated with the use of progestins are headache, depression, weight gain, and changes in libido 8
- 9. Contraceptives Contraception is the act of preventing pregnancy This can be a device, a medication, a procedure A. Major classes of contraceptive- Combination oral contraceptives: Products containing a combination of an estrogen and a progestin are the most common type of oral contraceptives Lippincott illustrated review Pharmacology, Sixth edition, page no.- 357 - 360 9
- 10. Transdermal patch: An alternative to combination oral contraceptives is a transdermal patch containing ethinyl estradiol and the progestin norelgestromin One contraceptive patch is applied each week for 3 weeks to the abdomen Injectable progestin: Medroxyprogesterone acetate is a contraceptive that is administered via intramuscular or subcutaneous injection every 3 months 10
- 11. Progestin implants: After subdermal placement, the etonogestrel implant offers contraception for approximately 3 years Vaginal ring: An additional contraceptive option is a vaginal ring containing ethinyl estradiol and etonogestrel The ring is inserted into the vagina and is left in place for 3 weeks and then removed 11
- 12. Mechanism of action Estrogen provides a negative feedback on the release of LH and follicle-stimulating hormone (FSH) by the pituitary gland, thus preventing ovulation Progestin also thickens the cervical mucus, thus hampering the transport of sperm 12
- 13. Adverse effect The most common adverse effects with estrogens are breast fullness, fluid retention, headache, and nausea Increased blood pressure may also occur Progestins may be associated with depression, changes in libido 13
- 14. THANK YOU 14