Essentials 1.2 Pharma Flashcards
(231 cards)
1
Q
What is the clinical use for Metformin?
A
Diabetes (Type II)
2
Q
What Class Does Glipizide Belong To?
A
Sulfonylureas
3
Q
What is the MOA of Glipizide?
A
It is Insulin secretagogue.
Glipizide binds to sulfonylurea receptor on β-cells and causes insulin secretion
4
Q
What Class Does Canagliflozin Belong To?
A
It is a Sodium-glucose co-transporter 2 (SGLT2) inhibitors
5
Q
A
6
Q
What is the MOA of Sodium-glucose co-transporter 2 (SGLT2) inhibitors?
A
Block reabsorption of glucose by SGLT 2 in the proximal tubule of the kidney causing glycosuria
7
Q
What Medications are SGLT2 Inhibitors
A
Canagliflozin
8
Q
What is the MOA of Sulfonylureas?
A
They Are insulin secretagogue. They function by binding to sulfonylurea receptors on β-cells and cause insulin secretion.
9
Q
What Medication is a Sulfonylureas?
A
Glipizide
10
Q
What is the MOA of Metformin
4 Main Principles
A
Reduces hepatic glucose production
Increase glucose absorption in muscle
Increase insulin sensitivity
Decrease intestinal glucose absorption
11
Q
What are Glucagon-like polypeptide-1 (GLP-1) receptor agonists?
A
They acts as analog of GLP1 which stimulates glucose-induced insulin secretion, suppresses glucagon, delays gastric emptying, and possibly improves beta cell function, causing weight loss
12
Q
What Medications are GLP1 Agonists?
A
Liraglutide and Semaglutide-
Think Medications ending in “-glutide”
13
Q
What is the MOA of Dipeptidyl peptidase-4 (DPP4 Inhibitors)?
A
Inhibits the enzyme that breaks down GLP-1, raising GLP-1 levels
14
Q
What Medications are DPP4 Inhibitors?
A
Sitagliptin
15
Q
What is the Mechanism of Actions of -Statins
A
Reversible competitive inhibitors of 3-hydroxy-3methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis.
This increases synthesis and reduces degradation of LDL receptors; therefore more LDL receptors on surface of hepatocytes=increased removal of LDL from blood
16
Q
What 3 Medications are the most commonly used -Statins
A
Rosuvastatin, Atorvastatin, Simvastatin
17
Q
What is the MOA of the drug class PCSK9 Inhibitors (Proprotein convertase subtilisin/kexin type 9)?
A
PCSK9 is a protein that binds to the LDL receptor, and reduces the LDL receptor density. This increases circulating LDL.
PCSK9 inhibitors are human monoclonal antibodies that block this process, increase LDL receptors and decrease circulating LDL.
18
Q
What Medications are PCSK9 Inhibitors?
A
Alirocumab
19
Q
What is the clinical use for Glipizide?
A
Diabetes (Type II)
20
Q
What is the clinical use for Canagliflozin?
A
Diabetes (Type II)
21
Q
What is the MOA of Fenofibrate
A
Agonist for the nuclear transcription factor PPAR-α which increases lipolysis and decreases triglycerides
22
Q
What is the MOA of Ezetimibe?
A
Selective inhibitor of cholesterol absorption from the small intestine via the sterol transporter NPC1L
23
Q
What is the MOA of Glucocorticoid Medications
A
Replaces endogenous cortisol and causes inhibition of phospholipase A2
This leads to↓ Cyclooxygenase (prostaglandins, leukotriene), Cytokines (Tumor necrosis factor, IL-3,4,5,13, Granulocyte-Macrophage Stimulating factor).
24
Q
What Medications act as Glucocorticoids?
A
Prednisone, prednisolone, hydrocortisone, dexamethasone
25
What is the MOA of Mineralocorticoid medications
Very potent affinity for mineralocorticoid receptor (↑ Na+/K+ATPase & ENaC expression) leads ↑ Na+ reabsorption and K+ excretion in distal tubules
25
What Medications act as Mineralcorticoids?
Fludrocortisone
25
What is the MOA of Ketoconazole?
Inhibits cytochrome P450-dependent enzymes and reduces cortisol synthesis
26
What is the MOA of the Medication Mitotane?
Cytotoxic drug that suppresses ACTH secretion and reduces synthesis of cortisol.
27
What is the MOA of Metyrapone?
Decreases cortisol synthesis by inhibition of 11-hydroxylase activity
28
What is the MOA of Levothyroxine (T4)?
Activation of various nuclear receptors in the body causing gene expression and protein synthesis.
29
What is the MOA of Propylthiouracil?
Inhibits both thyroid peroxidase reactions and 5'-deiodinase-used to manage hyperthyroidism.
30
What is the MOA of Methimazole?
Inhibits thyroid peroxidase reactions-used to manage hyperthyroidism.
31
What is the MOA of Potassium Iodide (SSKI) [aka Lugol's solution]?
Inhibits iodine organification and hormone release and reduces the size and vascularity of the thyroid gland
32
What is the MOA for Propranolol when used to for Hyperthyroidism?
Inhibition of β receptors, and inhibition of conversion of T4 to T3.
33
What is the clinical use for Liraglutide?
Diabetes (Type II)
34
What is the clinical use for Semaglutide?
(2 uses)
- Diabetes (Type II)
- Obesity
35
What is the clinical use for Sitagliptin?
Diabetes (Type II)
36
What is the clinical use for statins?
- High cholesterol levels
- High triglyceride levels
37
What is the clinical use for Fenofibrate?
- High cholesterol levels
- High triglyceride levels (mainly)
38
What is the clinical use for Ezetimibe?
- High cholesterol levels
39
What is the clinical use for Alirocumab?
- High cholesterol levels
40
What are the clinical uses for Prednisone, Prednisolone, Hydrocortisone, Dexamethasone?
(There are 7 main categories)
RARE DOG
- Rheumatologic
- Allergic
- Respiratory
- Endocrine
- Dermatologic
- Ophthalmic
- Gastrointestinal
41
What are the clinical uses for Fludrocortisone?
- Adrenal insufficiency
- Hypopituitarism
42
What is the off-label clinical use of Ketoconazole?
Cushing's syndrome
43
What is the clinical use of Mitotane?
(2; 1 on label, 1 off label)
- Inoperable adrenocortical carcinoma
- Cushing's syndromee (off label)
44
What is the off-label clinical use of Metyrapone?
Cushing's syndrome
45
What is the clinical use for Levothyroxine (T4)?
Hypothyroidism
46
What is the clinical use for Propylthiouracil (PTU)?
- Hyperthyroidism
47
What are the clinical uses for Methimazole?
(3)
- Hyperthyroidism
- 1st trimester of pregnancy
- thyroid storm
48
Between Propylthiouracil (PTU) & Methimazole which medication is preferred to to use in the 1st trimester of pregnancy & during a thyroid storm?
Methimazole
49
What are the clinical uses for Potassium Iodide (SSKI) [aka Lugol's solution]? (2)
- Preparation for surgical thyroidectomy
- Thyroid storm
50
What is the MOA of Somatropin?
It is a recombinant form of human Growth Hormone. Somatropin binds to Growth Hormone receptors and increases production of IGF-1.
Used to treat GH Deficiency
51
What is the MOA of Somatostatin analogs
Act as agonists at somatostatin receptors.
They inhibit production of GH and to a lesser extent, of TSH, glucagon, insulin, and gastrin.
52
What are 3 Somatostatin Analogs
Octreotide, Lanreotide, Pasireotide
53
What is the MOA of Pegvisomant?
Blocks GH receptors.
54
What is the MOA of the diuretic Spironolactone?
Acts as an aldosterone antagonist, increases Na and water excretion and decreases K excretion.
55
What is the MOA of the Loop Diuretic Furosemide?
Loop diuretic; It inhibits NKCC2 which reduces reabsorption of Na, Cl, K, Mg, and Ca
56
What is the MOA of Albumin?
It is a Colloid that increases intravascular oncotic pressure and causes mobilization of fluids from interstitial to intravascular space
57
What is the MOA of Alpha-1 Agonist Midodrine
Active metabolite is an alpha-1 agonist, which increases arteriolar and venous tone, resulting in increased blood pressure
58
What is the MOA of Octreotide?
Inhibits release of vasodilator hormones, leading to splanchnic vasoconstriction, decreased portal vein pressure, and decreased variceal pressure.
59
What is the MOA of Non-Selective Beta Blockers
Decrease cardiac output, which reduces portal pressure; produce splanchnic vasoconstruction, which reduces portal blood flow
60
What is the clinical use for Propranolol?
Thyroid storm
61
What Medications are Non-Selective Beta Blockers
Nadolol, Propranolol
62
What is the MOA of Nucleoside/Nucleotide Analogs
Used for Hepatitis B treatment. Prevents viral replication of Hepatitis by integrating synthetic nucleoside/nucleotides that result in a premature stop of encoded viral DNA
63
What Medications are Nucleoside/Nucleotide Analogs?
Entecavir, Lamivudine, Tenofovir
64
What is the MOA of NS5B Polymerase Inhibitors?
They inhibit the HCV NS5B RNA polymerase, which is essential for viral replication.
65
What Medications are NS5B Polymerase Inhibitors?
Dasabuvir, Sofosbuvir
66
What is the MOA of Ribavirin?
Interferes with the synthesis of guanosine triphosphate (GTP), inhibits capping of viral messenger RNA, inhibits viral polymerase
67
What is the MOA of Metoclopramide (Reglan)
D2-receptor antagonist
68
What is the MOA of Trimethobenzamide (Tigan)
"unknown, likely involves
the chemoreceptor
trigger zone"
69
What are the clinical uses for Somatropin? (4)
- Treatment of growth failure in children with GH deficiency, short stature, turner syndrome
- Chronic kidney disease
- Short bowel syndrome
- Wasting in HIV infection
70
Name three types of Somatostatin analogs:
1. Octreotide
2. Lanreotide
3. Pasireotide
71
What are the clinical uses for Somatostatin analogs?
- Acromegaly
- Hormone-secreting tumors
- Acute control of bleeding from esophageal varices (Octreotide)
72
What is the clinical use for Pegvisomant?
- Acromegaly (used in patients with inadequate response to surgery, radiation, or other therapies)
73
What is the clinical use for Spironolactone?
- Ascites
74
What drugs are best paired to rapidly reduce ascites?
- Furosemide & Spironolactone
75
What is the clinical use for Furosemide?
- Ascites
76
What are the clinical uses for Midodrine?
(3)
- Refractory ascites
- Hypotension with diuretic use
- Hepatorenal syndrome
77
What are the clinical uses for Albumin?
(2)
- Large volume paracentesis > 5 L
- Hepatorenal syndrome
78
What is the clinical use for Octreotide?
- Acute variceal bleeding, given for 3-5 days after variceal bleed
79
What is the clinical use for Nadolol & Propranolol?
- Used for primary & secondary prophylaxis of variceal bleeding
80
Which Drugs are used to treat Hep B? (5)
TEAL T
- Telbivudine
- Entecavir
- Adefovir
- Lamivudine
- Tenofovir
81
What is the MOA of 5-HT3 receptor antagonists
They block peripheral 5-HT3
receptors and 5-HT3
receptors in the vomiting
center
Used for Nausea
82
What Medications are 5-HT3 receptor antagonists
Ondansetron (Zofran)
83
What is the MOA of Neurokinin receptor
antagonists?
They block NK1 receptors in
the chemoreceptor
trigger zone.
84
What Medications are Neurokinin receptor
antagonists?
Aprepitant (Emend)
Fosaprepitant (Emend for
injection)
85
What is the MOA of Antipsychotics?
They inhibit dopamine and activation of
muscarinic receptors.
Used for Nausea
86
What Medications are Antipsychotics?
Prochlorperazine (Compazine)
Promethazine (Phenergan)
87
What is the MOA of Bulk-Forming Laxatives
Absorb water, forming a gel that distends the colon and promotes peristalsis.
88
What Medication is a Bulk-Forming Laxative?
Psyllium (Metamucil)
89
What is the MOA of Stool softeners?
Reduce surface tension of stool, allowing water and lipids to penetrate and soften.
90
What Medications Act as Stool Softeners?
Docusate (Colace)
91
What is the MOA of an Osmotic Laxative?
Nonabsorbable, cause osmotic retention of fluid in the colon, causing distension and increased peristalsis
92
What Medications act as Osmotic Laxatives?
Polyethylene glycol (Miralax)-Most Important
Lactulose (Enulose)
Magnesium hydroxide (Milk of Magnesia)
Magnesium citrate (Citroma)
Sodium phosphates (Fleet Enema)
93
What is the MOA of Stimulant Laxatives?
Stimulate the enteric nervous system, increase the rate of colonic motility, alter water and electrolyte secretion
94
What Medications act as Stimulant laxatives?
Bisacodyl (Dulcolax)
Senna (Senokot, Ex-Lax)
95
What is the MOA of Lubricant Laxatives?
Oil lubricates fecal material, preventing water resorption from the stool.
96
What Medications are Lubricant Laxatives?
Mineral oil (Fleet Oil)
97
What is the MOA of Opioid Receptor Antagonists?
block intestinal mu opioid receptors, it counteracts the constipating effects of opioids by restoring normal bowel movement function
Used for Constipation
98
What Medications Act as Opioid Receptor Antagonists?
Methylnaltrexone (Relistor)
Naloxegol (Movantik)
99
What is the MOA for Opioid agonists?
bind to opioid receptors in the intestines, inhibiting peristalsis and increasing transit time.
Used for Diarrhea
100
What Medications act as Opioid agonists?
Loperamide (Imodium)
Diphenoxylate/atropine (Lomotil)
101
What is the MOA of Bile acid Sequestrants?
They bind excess fecal bile acids.
By binding to excess bile acids, sequestrants prevent them from irritating the colon lining, thus reducing the frequency and severity of diarrhea.
102
What Medications act as Bile Acid Sequestrants?
Cholestyramine (Questran)
103
What is the MOA of Bismuth subsalicylate
It stimulates absorption of fluid and electrolytes across the intestinal wall, inhibits inflammation and hyper-motility.
104
What is the MOA of Lubiprostone (Amitiza)?
It stimulates chloride channels in the small intestine to help facilitate fluid excretion.
105
What is the MOA of Linaclotide (Linzess)?
Activates guanylyl cyclase-C, increasing cGMP and chloride-rich secretion to help facilitate fluid secretion.
106
What is the MOA of Eluxadoline (Viberzi)?
Is a mixed opioid agonist and antagonist to help make stools less loose and watery
107
What is the MOA of Rifaximin (Xifaxan)
Antibiotic, anti-inflammatory effects to help treat diarrhea caused by IBS.
108
What is the MOA of Aminosalicylates?
They reduce inflammation in the bowel from IBD by modulating inflammatory mediators, interfere with cytokine production, scavenges free radicals, inhibits natural killer cells, mucosal lymphocytes, and macrophages
109
What Medications are Aminosalicylates?
Mesalamine
Sulfasalazine
110
What is the MOA of Azathioprine
Suppresses your immune system by inhibiting DNA and RNA synthesis and limiting the proliferation of rapidly dividing immune cells, particularly lymphocytes
111
Which Drugs are used to treat Hep C? (2)
DR. S treats Hep C
- Dasabuvir
- Ribavirin
- Sofosbuvir
112
What is the clinical use for Metoclopramide (Reglan)?
- Nausea
113
What is the clinical use for Trimethobenzamide (Tigan) ?
- Nausea
114
What is the clinical use for Ondansetron (Zofran)?
- Nausea
115
What is the clinical use for Aprepitant (Emend)?
- Nausea
116
What is the clinical use for Fosaprepitant & how is it administered?
- Nausea
- Injection
117
What is the clinical use for Prochlorperazine (Compazine)?
- Nausea
118
What is the clinical use for Promethazine (Phenergan)?
- Nausea
119
What is the clinical use for Psyllium (Metamucil)?
- Constipation
120
What is the clinical use for Docusate (Colace)?
- Constipation
121
What is the clinical use for Polyethylene glycol (Miralax)?
- Constipation
122
What is the clinical use for Lactulose (Enulose)?
- Constipation
123
What is the clinical use for Magnesium hydroxide (Milk of Magnesia)?
- Constipation
124
What is the clinical use for Magnesium citrate (Citroma)?
- Constipation
125
What is the clinical use for Sodium phosphates (Fleet Enema)?
- Constipation
126
What is the clinical use for Bisacodyl (Dulcolax)?
- Constipation
127
What is the clinical use for Senna (Senokot, Ex-Lax)?
- Constipation
128
What is the clinical use for Mineral oil (Fleet Oil)?
- Constipation
129
What is the clinical use for Methylnaltrexone (Relistor)?
- Constipation
130
What is the clinical use for Naloxegol (Movantik)?
- Constipation
131
What is the clinical use for Loperamide (Imodium)?
- Diarrhea
132
What is the clinical use for Diphenoxylate/atropine (Lomotil)?
- Diarrhea
133
What is the clinical use for Cholestyramine (Questran)?
- Diarrhea
134
What is the clinical use for Bismuth subsalicylate? (5)
- Nausea
- Vomiting
- Upset stomach
- Diarrhea
- Quad Therapy for H. pylori
135
What is the MOA of Methotrexate
Inhibits dihydrofolate reductase, which inhibits the synthesis of purines and pyrimidines (inhibiting DNA and RNA synthesis of WBCs) producing anti-inflammatory effects.
136
What is the MOA of TNF Antagonists?
Are monoclonal antibodies that bind to TNF, preventing it from binding to its receptors and causing inflammatory effects.
137
What Medications are TNF Antagonists?
Infliximab (Remicade)
Adalimumab (Humira)
138
What is the MOA of Vedolizumab (Entyvio)
It is an Integrin receptor antagonist of white blood cells, preventing them from entering the gut lining and causing inflammation.
139
What is the MOA of Ustekinumab (Stelara)
Specifically targets and blocks the activity of IL-12 and IL-23. two proteins crucial for inflammatory processes in the body.
140
What is the MOA of the Antacids Medication Class?
They are weak bases, that react with protons in the lumen of the stomach to neutralize stomach acid.
141
What Medications belong to the Antacid Class?
Calcium Carbonate (Tums)
Magnesium Hydroxide
Aluminum Hydroxide
Sodium Bicarbonate
142
What is the MOA of the Histamine-2 Receptor Antagonists (H2RA) Class?
Competitive inhibition of gastric parietal cell H2 receptors preventing support of Parietal cell acid secretion.
143
What medications are part of the Histamine-2 Receptor Antagonists?
Famotidine
144
What is the MOA of Proton Pump Inhibitors (PPI)?
Irreversibly inactivate parietal cell proton pumps
145
What are the drugs used to treat occasional heartburn symptoms?
Fam SCAM
- Famotidine
- Sodium Bicarbonate
- Calcium Carbonate
- Aluminum Hydroxide
- Magnesium Hydroxide
146
What is the clinical use for Famotidine? (2)
- Occassional heartburn symptoms,
- Nighttime reflux in addition to a PPI
147
What are the clinical uses for Omeprazole? (5)
- GERD
- Erosive esophagitis
- PUD
- Prevention of NSAID-induced PUD
- Triple & Quad Therapy for H. pylori
148
What is the clinical use for Sucralfate?
- Duodenal ulcer treatment
149
What is the clinical use for Vonoprazan? (2)
- Erosive esophagitis,
- H. pylori treatment
150
What is the clinical use for Lubiprostone (Amitiza)?
- IBS
151
What is the clinical use for Linaclotide (Linzess)?
- IBS
152
What is the clinical use for Eluxadoline (Viberzi)?
- IBS
153
What is the clinical use for Rifaximin (Xifaxan)?
- IBS
154
What is the clinical use for Mesalamine &
Sulfasalazine?
- IBD
155
What is the clinical use for Azathioprine?
- IBD
156
What is the clinical use for Methotrexate?
- IBD
157
What is the clinical use for Infliximab (Remicade)
& Adalimumab (Humira)?
- IBD
158
What is the clinical use for Vedolizumab (Entyvio)?
- IBD
159
What is the clinical use for Ustekinumab (Stelara)?
- IBD
160
What are the clinical uses for Leuprolide? (2)
- Endometriosis
- Prostate cancer
161
What is the clinical use for Danazol?
- Endometriosis
162
What are the clinical uses for Anastrozole? (primary, secondary, & off label)
- Breast cancer (primary)
- Endometriosis (secondary)
- Infertility (Off label)
163
What is the clinical use for Clomiphene?
- Anovulatory infertility
164
What is the clinical use for hCG, choriogonadotropin alfa?
- Infertility
165
What are the clinical uses for estrogen receptor agonists?
- Menopausal Symptoms
i.e. Hot flashes & vaginal dryness
166
What Medications are PPIs?
Omeprazole
167
What is the MOA of Sucralfate?
Forms a viscous paste in acidic solutions that binds selectively to ulcers or erosions, stimulates mucosal prostaglandin and bicarbonate secretion.
Protects Stomach Mucosa
168
What is the MOA of Bismuth compounds?
Coats ulcers and erosions, may stimulate prostaglandin, mucus, and bicarbonate secretions.
169
What Drug is a Potassium-competitive acid inhibitors (PCABs)?
Vonoprazan
170
What is the MOA of Vonoprazan?
Competes for potassium on the luminal side of the parietal cell and causes rapid and reversible inhibition of parietal cell proton pumps.
171
Name the H. Pylori Triple Therapy
PPI, amoxicillin, clarithromycin (Biaxin®),
172
Name the H. Pylori Quadruple Therapy
PPI, bismuth subsalicylate, metronidazole (Flagyl®), and tetracycline
173
What is the MOA of Prazosin?
It is a competitive antagonism at α1 receptors relaxes bladder smooth muscle.
174
What is the MOA of Tamsulosin?
It is a competitive antagonism at α1 receptors relaxes bladder smooth muscle.
175
What is the MOA of Doxazosin, Terazosin, Silodosin?
It is a competitive antagonism at α1 receptors relaxes bladder smooth muscle.
176
List estrogen receptor agonists: (4)
- Estradiol
- Conjugated estrogens
- Esterified Estrogens
- Estropipate
177
What is the clinical use for Raloxifene?
- Postmenopausal osteoporosis
178
What is the clinical use for Testosterone?
- Hypogonadism
i.e. low energt & libido
179
What is the clinical use for Flutamide?
- Prostate cancer
180
What is the clinical use for Bicalutamide?
- Prostate cancer
181
What are the clinical uses for Prazosin? (2)
- Benign prostatic hyperplasia
- Hyperplasia
182
What is the MOA of Finasteride, Dutasteride?
They are 5α-Reductase Inhibitors, block conversion of DHT to Testosterone which helps prevents further prostatic bladder hyperplasia.
183
What is the MOA of Anticholinergic Medications for Overactive Bladder?
Direct antispasmodic action on smooth muscle by blocking muscarinic acetylcholine receptors on bladder preventing smooth muscle contraction.
184
What is the MOA of PDE5 Inhibitors?
PDE5 inhibitors, inhibit enzyme that degrades cGMP, which leads to smooth muscle relaxation, increased blood flow, and erection.
185
What Medications are PDE5 Inhibitors?
Sildenafil, tadalafil, vardenafil (To -fil the penis) 🍆
186
What is the MOA of Leuprolide?
GnRh agonists-
Stimulates release of pituitary gonadotropins, FSH and LH, resulting in a temporary increase in gonadal hormone synthesis but with continued dosing eventual suppression of release.
For Men used for hormonal suppression of prostate cancer.
For Women used to help manage Endometriosis
187
What are the clinical uses for Doxazosin? (2)
- Benign prostatic hyperplasia
- Hyperplasia
188
What are the clinical uses for Terazosin? (2)
- Benign prostatic hyperplasia
- Hyperplasia
189
What is the clinical use for Tamsulosin?
- Benign prostatic hyperplasia
190
What is the clinical use for Silodosin?
- Benign prostatic hyperplasia
191
What are the clinical uses for Finasteride? (2)
- Benign prostatic hyperplasia
- Male Pattern Baldness
192
What are the clinical uses for Dutasteride? (2)
- Benign prostatic hyperplasia
- Male Pattern Baldness
193
What is the clinical use for oxybutynin?
- Symptoms associated with overactive bladder
194
What is the clinical use for tolterodine?
- Symptoms associated with overactive bladder
195
What is the clinical use for trospium?
- Symptoms associated with overactive bladder
196
What are the clinical uses for Sildenafil?
- Erectile Dysfunction
- Pulmonary arterial hypertension
197
What are the clinical uses for Tadalafil?
- Erectile Dysfunction
- Pulmonary arterial hypertension
198
What are the clinical uses for Vardenafil?
- Erectile Dysfunction
- Pulmonary arterial hypertension
199
What is the clinical use for Misoprostol?
- Medical abortion up to 10-13 weeks gestation
200
What is the MOA of Danazol?
Androgen agonist.
Also has some progestin agonist and anti-estrogen activity.
Results in suppression of pituitary-ovarian access.
Causes Pseudo-menopause.
Used for Endometriosis
201
What is the MOA of Anastrozole?
Inhibits conversion of androstenedione and testosterone to estrone and estradiol, prevents endometrial thickening.
202
What is the MOA of Clomiphene (Hint #twinning🤰)
Clomiphene is a selective estrogen receptor modulator (SERM)
It inhibits estradiol's negative feedback on GnRH, FSH and LH-increasing their secretion, leading to ovulation.
203
What is the MOA of hCG, choriogonadotropin alpha (Hint#Preganananat🤰)
Stimulates ovulation after use of an FSH analog to stimulate follicular development and trigger their final maturation and ovulation.
Acts as a "trigger" to release a mature egg from the dominant follicle by mimicking the natural LH surge, which is necessary for ovulation to occur; this happens when a follicle is sufficiently developed and has acquired LH receptors on its granulosa cells.
204
What is the MOA of Estradiol, Conjugated estrogens, Esterified Estrogens, Estropipate?
Estrogen receptor agonists. Estradiol is bio-identical.
205
What is the MOA of Medroxyprogesterine (Depo-Shot), norethindrone (Mini-pill), micronized progesterone?
Progesterone receptor agonists. Micronized progesterone is bio-identical.
206
What is the clinical use for Mifepristone?
- Medical abortion up to 10-13 weeks gestation
207
What are the clinical uses for Methotrexate? (2)
- Abortion of ectopic pregnancy
- Moderate IBD
208
What is the clinical use for Levonorgestrel?
- Pregnancy Prevention
209
What is the MOA of Raloxifene?
This is a Selective estrogen receptor modulator (SERM)
Helps prevents the thinning of bone in post-menopausal women by acting as an Estrogen agonist at the vaginal tissues and bone.
Acts as an Estrogen antagonist at the breast tissue and prevents breast tissue proliferation.
Helps with reducing risk of breast cancer in menopausal women.
210
What is the MOA of Testosterone?
Testosterone receptor agonist; It is "bio-identical."
211
What is the MOA of Mifepristone
Progesterone receptor competitive antagonist, and breaks down the connection of implanted egg on uterine wall.
212
What is the MOA of Mifepristone
Prostaglandin analogue that induces cervical contractions and facilitates removal of uterine contents.
213
What is the MOA of Methotrexate
Inhibits dihydrofolate reductase, producing anti-inflammatory effects used in autoimmune diseases.
Was commonly used for therapeutic abortion (1st trimester) before mifepristone was approved.
Still used in select cases for abortion of ectopic pregnancy
214
What is the MOA of Menotropins (purified hMG)?
FSH:LH in a 1:1 ratio--stimulates follicular growth and maturation and stimulates ovulation.
215
What is the MOA of Follatropin Alpha, Follatropin Beta, and Urofollitropin?
Stimulates follicular growth and maturation and act as FSH analogs.
Directly stimulate the maturation of ovarian follicles by promoting their growth and development
Allowing multiple follicles to reach maturity simultaneously
216
What is the MOA of Combination Oral Contraception:
Estrogen: inhibition of FSH release leads to inhibition of the development of dominant follicle, and thus inhibition of ovulation.
It stabilizes endometrium to improve bleeding patterns (for reduced adverse effects).
Progestin: decreases tubal motility-i.e. fimbriae do not wrap around the ovaries, increases cervical mucous viscosity, thins or prevents endometrium formation, and inhibits ovulation through negative feedback.
217
What Medications Make up Combined Oral Contraceptives
estrogen/progestin:
Ethinyl estradiol/drospirenone (Yaz, Yasmin)
Thinyl esetradiol/norgestimate (Ortho Cyclen, Ortho Tri-cyclen).
Estrogens: ethinyl estradiol, mestranol.
Progestins: desogestrel, levonorgestrel, norgestimate, norethindrone, drospirinone
218
What is the MOA of Progestin only Contraceptives?
Progestin: decreases tubal motility-i.e. fimbriae do not wrap around the ovaries, increases cervical mucous viscosity, thins or prevents endometrium formation, and inhibits ovulation through negative feedback.
219
What is the MOA of Levonorgestrel (Plan B Medication)
Plan B works by delaying ovulation and follicular development and prevent pregnancy if given in a timely manner after unprotected intercourse (72-120 hours). If pregnancy already implanted, no effect.
Increasing your progestin levels causing negative inhibition of GnRH which keeps FSH and LH low, preventing follicle proliferation by ensuring no estradiol production.
220
What is the MOA of the Copper Intrauterine Device
Spermicidal
221
What is the MOA Levonorgestrel (IUD)?
Functions by increasing progestin levels which thickening cervical mucus to prevent sperm from reaching an egg, prevents building the uterine lining, keeping it thin which make implantation less likely, and inhibiting ovulation by preventing an egg from fully developing
Increasing your progestin levels causing negative inhibition of GnRH which keeps FSH and LH low, preventing follicle proliferation by ensuring no estradiol production.
(Potentially less consistent effect on ovulation than progestin)
222
What Medications are Progestin Only Contraceptive
Oral: norethindrone, norgestrel (Mini-Pill.
Injectable Depo Shot (depomedroxyprogesterone).
Implant: 3-ketodesogestrel (Nexplanon)
223
What forms does Levonorgestrel come in? (2)
- Hormonal IUD
- Oral Hormonal Emergency Contraception
224
What are the clinical indications for a combined oral contraceptive (COC)?
- Pregnancy prevention
- Control of PMS symptoms
- Improvement in menorrhagia
- Improvement in acne
225
Which forms of contraception are indicated when estrogens are contraindicated?
List the hormone & 3 different contraceptive options.
Hormone: Progesterone/Progestin
Contraceptive options:
1. Norethindrone (Oral)
2. Depomedroxyprogesterone (injection)
3. Nexplanon (Implant)
226
What are the main contraindications (5) for combined oral contraceptives? What is the hormone?
Hormone: Estrogen
1. Coagulopathy
2. Hx of clots (DVT & PE)
3. >35 years old & smoking
4. 6 weeks past partum
5. Migraine w/ Aura
227
What contraceptive is contraindicated in a patient with Wilson's Disease?
Copper IUD
228
What is the clinical use for Menotropins (purified hMG)?
- Infertility
229
What is the clinical use for Follatropin Alfa, Follatropin Beta, Urofollitropin
- Infertility
