block 8 drugs

Question 1

Testosterone

Question 2

Sildenafil

Question 3

Bicalutamide

Answer 3

Class: androgen receptor inhibitor

Indication: Stage D2 metastatic carcinoma of the prostate. Given in combination with luteinizing hormone-releasing hormone (LHRH) agonist .

Mechanism:
Bicalutamide competes with androgen for the binding of androgen receptors,

Question 4

Finasteride

Answer 4

Class: antiandrogenic ( 5a reductase inhibitor)

Indication:
- benign prostatic hyperplasia
- hair loss in males

Mechanism:
inhibits type 5a reductase. Which is needed to convert androgen testosterone into 5α-dihydrotestosterone (DHT)

Question 5

Goserelin

Answer 5

Class:
- LH (luteinizing hormone) blocker

Indication:
- used to treat breast cancer and prostate cancer by reducing secretion of gonadotropins (LH) from the pituitary.
- In males decreases production of testosterone
- In females decreases production of estrogen

Question 6

Ethinylestradiol

Answer 6

class: synthetic estradiol (estrogen)

Indication:
- used as a contraceptive
- premenstrual dysphoric disorder
- moderate acne
-moderate to severe vasomotor symptoms of menopause
-prevention of postmenopausal osteoporosis

Mechanism:
- decreases LH

Question 7

Tamoxifen

Answer 7

Class: selective estrogen receptor modulator (SERM) Estrogen receptor competitor

Indicator:
- treat estrogen receptor positive breast cancers
- as well as prevent the incidence of breast cancer in high risk populations

Question 8

HRT

Question 9

Artificial progesterone

Answer 9

Progesterone is a hormone that occurs naturally in females, and is essential for endometrial receptivity, embryo implantation, and the successful establishment of pregnancy.

A low progesterone concentration or an insufficient response to progesterone can cause infertility and pregnancy loss

Indication:

• including contraception
• control of abnormal uterine bleeding
  -maintenance of pregnancy
• prevention of endometrial hyperplasia.

Progesterone is available in gelatinized capsule form, vaginal gel form, tablet form, vaginal insert form, and injection form

Question 10

Medroxyprogesterone

Answer 10

Drug class: Progesterone derivative

Indications:
-secondary amenorrhea
- abnormal uterine bleeding
-pain from endometriosis
- endometrial and renal carcinomas
- paraphilia in males
- GnRH-dependent precocious puberty.

Mechanism:
- inhibits gonadotropin production
-reduces nuclear estrogen receptors and DNA synthesis in epithelial cells of the endometrium
- induces p53 dependant apoptosis in cancer cell lines

Question 11

Norithisterone

Answer 11

class: synthetic second-generation progestin

Indication:
-contraception
- prevention of endometrial hyperplasia in hormone replacement therapy

Question 12

Mefenamic acid

Answer 12

Drug class: NSAID

Indications: Mefenamic acid is an NSAID used to treat mild to moderate pain for no more than a week, and primary dysmenorrhea.

Question 13

Tranexamic acid

Answer 13

Drug class: antifibrinolytic

Indications:
- heavy menstrual bleeding in premenopausal women
- hereditary angioedema
-

Question 14

Clomiphene

Answer 14

Drug class: SERM ( selective estrogen modulator )

Indication:
Clomifene is a medication used to induce ovulation.

Mechanism:
-Clomifene appears to stumulate the release of gonadotropins, follicle-stimulating hormone (FSH), and leuteinizing hormone (LH), which leads to the development and maturation of ovarian follicle, ovulation, and subsequent development and function of the coprus luteum, thus resulting in pregnancy

Question 15

Oxytocin

Answer 15

Indication: Oxytocin is a recombinant hormone used to induce or strengthen uterine contractions in pregnant women to aid in labor and delivery or to control postpartum bleeding.

Mechanism:
-Oxytocin plays a vital role in labour and delivery.
he hormone is produced in the hypothalamus and is secreted from the paraventricular nucleus to the posterior pituitary where it is stored.
It is then released in pulses during childbirth to induce uterine contractions.

Question 16

Orlistat

Answer 16

Drug class: inhibits gastrointestinal lipases

Indication: Orlistat is a reversible inhibitor of gastrointestinal lipases indicated for weight loss and weight maintenance.

Mechanism: When orlistat is taken with food containing fat, it partially inhibits the hydrolysis of triglycerides. This decreases absorption of monoaclglycerides and free fatty acids, contributing to weight maintenance and weight loss

Question 17

Liraglutide

Answer 17

Drug class: GLP-1 analog

Indication:
- weight loss
- weight management

Mechanism:
- is similar (an analog) of synthetic glucagon-like peptide-1 analog
- Liraglutide is an agonist of the glucagon-like peptide-1 receptor which is coupled to adenylate cyclase
- The increase in cyclic AMP stimulates the glucose dependant release of insulin, inhibits the glucose dependant release of glucagon, and slows gastric emptying to increase control of blood sugar

Question 18

Gliclazide

Answer 18

Drug class: sulfonylurea

Indication:
- used to treat hyperglycemia in patients with type 2 diabetes mellitus.
- non-insulin-dependent diabetes mellitus (NIDDM)

Mechanism:
-Gliclazide binds to the β cell sulfonyl urea receptor (SUR1). –This binding subsequently blocks the ATP sensitive potassium channels.
-The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the β cells.
- This opens voltage-dependent calcium channels in the β cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.

Question 19

Repaglinide

Answer 19

Drug class: antihyperglycemic
meglitinide

Indication:
- Repaglinide is a antihyperglycemic used to improve glycemic control in diabetes.
- Thee treatment of non-insulin-dependent diabetes mellitus (NIDDM).

Mechanism:
- by binding to β cells of the pancreas to stimulate insulin release.
- Repaglinide induces an early insulin response to meals decreasing postprandial blood glucose levels.

Question 20

Glucagon

Answer 20

Indication:
- glucagon used to treat hypoglycemia in diabetes mellitus

Mechanism:
- Glucagon binds to the glucagon receptor activating Gsα and Gq.1
- This activation activates adenylate cyclase, which increases intracellular cyclic AMP and activates protein kinase A
-

Question 21

Insulin

Answer 21

Indication: hyperglycemia in diabetes mellitus.

Mechanism:
-Insulin promotes glucose and amino acid uptake into muscle and adipose tissues,

-Insulin inhibits gluconeogenesis in the live

Question 22

Exanatide

Answer 22

Drug class: GLP-1 agonist

Indication: Exenatide is a GLP-1 agonist used in the management of type 2 diabetes mellitus.

Mechanism:
Exenatide is a human glucacon-like peptide-1(GLP-1) receptor agonistLabel. By activating this receptor, insulin secretion is increased and glucagon secretion is decreased in a glucose dependant manner

Question 23

Sitagliptin

Answer 23

Drug class: oral dipeptidyl peptidase-4 (DPP-4) inhibitor

Indication:
-to improve glycemic control in adults with type 2 diabetes mellitus.
- It is not used to treat type 1 diabetes or patients with a history of pancreatitis.

Mechanism:
-Inhibition of DPP-4 by sitagliptin slows DPP-4 mediated inactivation of incretins like GLP-1 and GIPLabel,2.
-Incretins are released throughout the day and upregulated in response to meals as part of glucose homeostasisLabel,4. Reduced inhibition of incretins increase insulin synthesis and decrease glucagon release in a manner dependant on glucose concentrations.
- These effects lead to an overall increase in blood glucose control which is demonstrated by reduced glycosylated hemoglobin (HbA1c

Question 24

Dapagliflozin

Answer 24

Drug class: sodium-glucose cotransporter 2 inhibitor

Indication: to improve glycemic control in adult patients with type 2 diabetes mellitus along with diet and exercise

Mechanism:
-Dapagliflozin inhibits the sodium-glucose contransporter 2(SGLT2) which is primarily located in the proximal tubule of the nephron1.
-SGLT2 facilitates 90% of glucose reabsorption in the kidneys and so its inhibition allows for glucose to be excreted in the urine1.
-This excretion allows for better glycemic control and potentially weight loss in patients with type 2 diabetes mellitus

Question 25

Metformin

Answer 25

Drug class: biguanide antihyperglycemic

Indication: glycemic control in type 2 diabetes mellitus.

Mechanism:
-Metformin decreases blood glucose levels by decreasing hepatic glucose production (also called gluconeogenesis), decreasing the intestinal absorption of glucose, and increasing insulin sensitivity by increasing peripheral glucose uptake and utilization.
- It is well established that metformin inhibits mitochondrial complex I activity, and it has since been generally postulated that its potent antidiabetic effects occur through this mechanism.
-The above processes lead to a decrease in blood glucose, managing type II diabetes and exerting positive effects on glycemic control.

Question 26

Pancretin

Question 27

Pioglitazone

Answer 27

Drug class: thiazolidinedione

Indication:
- improve glycemic control in adults with type 2 diabetes mellitus

Mechanism:

-Pioglitazone is a selective agonist at peroxisome proliferator-activated receptor-gamma (PPARγ) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver.
- Activation of PPARγ increases the transcription of insulin-responsive genes involved in the control of glucose and lipid production, transport, and utilization.
- Through this mechanism, pioglitazone both enhances tissue sensitivity to insulin and reduces the hepatic production of glucose (i.e. gluconeogenesis) - insulin resistance associated with type 2 diabetes mellitus is therefore improved without an increase in insulin secretion by pancreatic beta cells.

Question 28

Acarbose

Answer 28

Drug class: alpha-glucosidase inhibitor

Indication: management of glycemic control in patients with type 2 diabetes mellitus.

Mechanism:
- Alpha-glucosidase enzymes are located in the brush-border of the intestinal mucosa and serve to metabolize oligo-, tri-, and disaccharides (e.g. sucrose) into smaller monosaccharides

• Acarbose is a complex oligosaccharide that competitively and reversibly inhibits both pancreatic alpha-amylase and membrane-bound alpha-glucosidase

Question 29

Bromocriptine

Answer 29

Drug class: dopamine D2 receptor agonist

Indication:
-treatment of galactorrhea due to hyperprolactinemia other -prolactin-related conditions
-early Parkinsonian Syndrome.

Question 30

Cabergoline

Answer 30

Drug class: dopamine receptor agonist

Indication: treatment of hyperprolactinemic conditions due to various causes.

Question 31

Carbimazole

Answer 31

Drug class:

Indication:
- Carbimazole is a drug used for the reduction of thyroid function.

Mechanism:

-Carbimazole is an aitithyroid agent that decreases the uptake and concentration of inorganic iodine by thyroid, it also reduces the formation of di-iodotyrosine and thyroxine.
-Once converted to its active form of methimazole, it prevents the thyroid peroxidase enzyme from coupling and iodinating the tyrosine residues on thyroglobulin, hence reducing the production of the thyroid hormones T3 and T4.

Question 32

Levothyroxine

Answer 32

Drug class: synthetic T4 hormone

Indication:
- used to treat hypothyroidism that can be used along with surgery
- radioiodine therapy to manage thyrotropin-dependent well-differentiated thyroid cancer.

Question 33

Desmopressin

Answer 33

Drug class: synthetic analog of vasopressin

Indication:
- used to reduce renal excretion of water in central diabetes insipidus and nocturia.

Mechanism:
-Upon binding of desmopressin to V2 receptors in the basolateral membrane of the cells of the distal tubule and collecting ducts of the nephron, adenylyl cyclase is stimulated.
- The resulting intracellular cascades in the collecting duct lead to increased rate of insertion of water channels, called aquaporins, into the lumenal membrane and enhanced the permeability of the membrane to water 6.

Question 34

Somatropin

Answer 34

Drug class: recombinant human growth hormone

Indication:
-Somatotropin is indicated for the treatment of pediatric patients who have growth failure due to an inadequate secretion of endogenous growth hormone, short stature associated with Turner syndrome, Prader-Willi syndrome (PWS)

Question 35

Octreotide

Answer 35

Drug class: peptide drug used to treat acromegaly

Indication:
- Octreotide by injection is used for the treatment of acromegaly and the reduction of flushing and diarrhea symptoms related to carcinoid tumors and/or vasoactive intestinal peptide (VIPoma) tumors.
The delayed-release oral formulation is used for the long-term treatment of acromegaly in patients who tolerate and respond adequately to injectable octreotide and lanreotide

Mechanism:

-Octreotide binds to somatostatin receptors coupled to phospholipase C through G proteins and leads to smooth muscle contraction in the blood vessels.

-Downstream effects that stimulate phospholipase C, the production of 1, 4,5-inositol triphosphate, and action on the L-type calcium channels lead to the inhibition of growth hormone, treating the various growth-hormone and metabolic effects of acromegaly.

Question 36

Sildenafil

Answer 36

Sildenafil is a phosphodiesterase inhibitor

Indication: used for the treatment of erectile dysfunction.

Mechanism:
smooth muscle relaxation and vasodilation increased flow of blood into the spongy erectile tissue of the penis that consequently allows it to grow in size and become erect and rigid

• stops the breakdownof cyclic guanosine monophosphate (cGMP)
• by inhibiting phosphodiesterase type 5 (PDE5)