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Endo Pharm Flashcards

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1
Q

Metformin

A

MOA: Decreases hepatic glucose production

PK: rapidly absorbed in small intestine (no liver metabolism), excreted unchanged in urine. t1/2= 4-9 hours. Takes 2 weeks for maximal effect

Side effects: GI (30% patients, only 5% stopped meds); lactic acidosis (rare, high fatality rate); reduced vitamin B12 (30%, but rarely causes anemia)

Contraindications: renal disease (creatinine greater than 1.5), active liver disease (lactic acidosis risk), discontinue with iodinated contrast medium administration

Uses: Lowers A1C 1-2%; mild weight loss; prevents diabetes in pre-diabetics; favorable lipid effects (small); decreased CV disease, malignancies

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2
Q
  • Glipizide
  • Glyburide
  • Glimepiride
  • Tolbutamide
  • Chlorpropamide
A

Sulfonylureas

MOA: bind to sulfonylurea receptor to block K+ exit from beta-cell–> Ca+2 release–> insulin release

PK: Kidney exretion

Side effects: Hypoglycemia (most common), mild weight gain, dizziness, headache, nausea (rare)

Contraindications: Patients at risk of hypoglycemia; sulfonamide allergy (sulfa antibiotics)

Uses: lower A1C 1-2%; works quickly; long term failure in 30% patients; flat dose-response relationship (max response at 1/2 maximal dose); NO improvement in insulin resistance or CV risk factors

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3
Q

Repaglinide

A

Meglitinides
Slightly different structure, receptor than sulfonylureas, but same MOA. Shorter half life

Advantages: less hypoglycemia than sulfonylureas (act quicker, degrade faster)

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4
Q

Rosiglitazon (Avandia)

A

Thiazolidinediones
MOA: increase insulin sensitivity by stimulating PPAR gamma:
- Promotes differentiation of small, metabolically active adipocytes
- Alters level of secretory products (reduces TNF and FFA)
- Raises adiponectin
- Alters adipose tissue distribution (shifts visceral fat to subcutaneous distribution)
Leads to improved insulin action, glucose metabolism, vascular function

  • Rosiglitazone associated with increased risk of ischmic cardiac events–> restricted use
  • Full clinical effect is slow (2-4 moths) due to alterations in adipocytes/fat distribution
  • Won’t cause hypoglycemia

PK: liver metabolism; biologic half life= hours, pharmacologic= months

Side effects: peripheral edema (4-6%); weight gain (2-3 kg over 1 year); osteoporosis; hepatotoxicity (rare); macular edema (rare)

Clinical use: lower A1c .5-1.4% (small glucose lower effects)

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5
Q

Acarbose

A

Alpha-glucosidase inhibitors

MOA: inhibit upper GI enzymes that convert complex polysaccharide carbs into monosaccharides (slow absorption of glucose, slower rise in postprandial blood glucose

Side effects: GI (GAS!)

Clinical use: only lowers A1C 0.5%, dosed 3 times/day, low hypoglycemia risk, RARELY USED due to weak glucose lowering effects plus bad side effects

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6
Q

Exenatide

A

MOA: synthetic version of Gila monster salivary protein; binds to GLP-1 receptors on beta cells–> stimulates insulin secretion, inhibits glucagon, slows gastric emptying, causes early satiety

PK: minimal systemic metabolism; proteolytic degradation; exenatide t1/2= 2-4 hours, liraglutide 1/2= 13 hours

Side effects: Nausea (suppresses appetite), jittery/dizzy, headache, pancreatitis, renal failure (do not use with renal clearance < 30), c-cell tumors (contraindicated in medullary thyroid cancer/MEN-2)

Clinical use: decrease in A1c 0.5-1.2%, weight loss (5-10 lbs), exenatide dose with meals (liraglutide dosed 2 times/day)

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7
Q

Gliptins

A

MOA: DPP-4 Inhibitor= inhibit dipeptidyl peptidase-4, thus blocking breakdown of GLP-1/GIP

Side effects: nasopharyngitis, URI, headache, pancreatitis, hypersensitivity rxn

Clinical use: lower A1c 0.5%-0.9%, once daily, weight neutral, low hypoglycemia risk

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8
Q

Pramlintide

A

MOA: analog of amylin inhibiting glucagon secretion, slows gastric emptying (delays absorption of carbs)

Side effects: nausea, hypoglycemia

Clinical use: insulin treated DM (sub-q injection before meals- lower insulin to prevent hypoglycemia), lowers A1c 0.5-0.6%, mild weight loss

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9
Q

Colesevalam

A

MOA: bile acid sequestrant

Side effects: GI

Clinical use: lowers A1c 0.5%; needs to be taken as powder or 6 pills/day

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10
Q

Sermorelin

A

1st 29 aa of native GHRH

  • Clinical uses: diagnosis of pituitary dwarfism (in children of short stature): administration should increase GH in hypothalamic GHRH defect
  • Administered IV/SC; 12- minute half-life
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11
Q

Hexarelin

A

6 aa native GHRH

  • Clinical uses: diagnosis of pituitary dwarfism (in children of short stature): administration should increase GH in hypothalamic GHRH defect
  • Administered intranasally
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12
Q

Growth hormone: somatotropin/somatrem

A

Promotes growth of long bones, muscle growth (anabolic), lipolysis, increased plasma glucose by binding GH single-transmembrane receptors

  • Somatotropin= animal-derived bHG
  • Somatropin/somatrem= rDNA HGH

Clinical uses: replacement therapy for:

  • Attaining satisfactory height (until epiphyseal plate closure) in GH-deficiency dwarfism (<4cm/year)
  • Long-term treatment of adults with idiopathic short stature
  • Reverse catabolic states (AIDS, wasting)
  • Improved GI function in short bowel syndrome

Adverse effects: diabetes, hypothyroidism, carpal tunnel syndrome, swelling

Contraindications: Praeder-Willi syndrome (respiratory problems); active tumors/hx tumors; growth promotion in pts with closed epiphyseal plates

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13
Q

Mecasermin

A

Recombinant human IGF-1 and human insulin-like growth factor binding protein-3

Uses: children with growth factor, IGF-1 deficiency who are not responsive to GH (mutation in GH receptor, antibodies against GH)

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14
Q

Pegvisomant

A

Growth hormone receptor antagonist: PEG derivative of mutant GH with altered receptor-binding properties

Uses: second line therapy for treating acromegaly (after surgery)

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15
Q

Octreotide

A

Somatostatin analog: decreases GH release from anterior pituitary; inhibits release of gastrin, pepsin, glucagons, gastric acid

IM slow release (monthly)

Uses:

  • reduce GH in acromegaly patients
  • gastrinoma/glucagonoma and severe diarrhea (diabetic, secretory)

Adverse effects: GI, biliary, cardiac (bradycardia), glucose intolerance, B12 deficiency

Contraindications: hepatic, renal impairment

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16
Q

Lanreotide

A

Somatostatin analog: decreases GH release from anterior pituitary

Uses: indicated for acromegaly

Adverse effects: GI, biliary, cardiac (bradycardia), glucose intolerance, B12 deficiency

Contraindications: hepatic, renal impairment

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17
Q

Bromocriptine

A

Oral dopamine agonist:

  • Decrease release of prolactin
  • Lowers neurotransmitter activities that induce/maintaining glucose-resistant state of diabetes
  • Oral medication

Uses:

  • Treat hyperprolactinemia related to prolactinoma (galactorrhea, hypogonadism)
  • Inhibit post-partum lactation
  • DM: weak glucose-lowering effect (A1c 0.5%), decrease CV disease

Side efects: nausea, light-headedness, orthostatic hypotension, constipation

Contraindications: uncontrolled hypertension, ischemic heart disease, PVD, history of schizophrenia (dopaminergic)

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18
Q

Cabergoline

A

Oral dopamine agonist: decrease release of prolactin

  • longer half-life than bromocriptine, more effective binding, less nausea/GI side effects

Uses:

  • Treat hyperprolactinemia related to prolactinoma
  • Inhibit post-partum lactation

Side efects: nausea, light-headedness, orthostatic hypotension, constipation

Contraindications: uncontrolled hypertension, ischemic heart disease, PVD, history of schizophrenia (dopaminergic)

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19
Q

Aqueous Vasopressin

A

Synthetic vasopressin mimicking effects of ADH: increased water resorption

  • short-acting version: 3-6 hours
  • Administered IM, IV, SC
    Uses: transient diabetes insipidus

Side effects:

  • Nausea, HA, cramping
  • Hyponatremia
  • Vasopressor on coronary vessels in large doses–> angina

Contraindications: moderate to severe renal impairment, history of hyponatremia

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20
Q

Vasopressin tannate in oil

A

Synthetic vasopressin mimicking effects of ADH: increased water resorption

  • long-acting: 24-72 hours
  • IM administration

Uses: Diabetes insipidus, esophageal varocele bleeding, colonic diverticular bleeding

Side effects:

  • Nausea, HA, cramping
  • Hyponatremia
  • Vasopressor on coronary vessels in large doses–> angina

Contraindications: moderate to severe renal impairment, history of hyponatremia

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21
Q

Lysine vasopressin

A

Synthetic vasopressin mimicking effects of ADH: increased water resorption

  • short-acting: 4-6 hours
  • Nasal spray administration

Uses: Diabetes insipidus, esophageal varocele bleeding, colonic diverticular bleeding

Side effects:

  • Nausea, HA, cramping
  • Hyponatremia
  • Vasopressor on coronary vessels in large doses–> angina

Contraindications: moderate to severe renal impairment, history of hyponatremia

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22
Q

Desmopressin (DDAVP)

A

Synthetic vasopressin mimicking effects of ADH: increased water resorption

  • Oral medication

Uses: Diabetes insipidus, esophageal varocele bleeding, colonic diverticular bleeding, NO LONGER used forPrimary nocturnal enuresis (PNE)

Side effects:

  • Nausea, HA, cramping
  • Hyponatremia (Desmopressin= CONTRAINDICATION)
  • Vasopressor on coronary vessels in large doses–> angina

Contraindications: moderate to severe renal impairment, history of hyponatremia

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23
Q

Demeclocycline

A

Tetracycline used for SIADH (syndrome of inappropriate ADH secretion)

  • Oral administration
  • Antagonizes ADH on renal tubules
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24
Q

Conivaptan

A

SIADH med: Vasopressin receptor antagonist used in euvolemic hyponatremia (blocks effects of ADH causing water retention)

  • CYP3A4 inhibitor
  • Adverse effects: hypokalemia, orthostatic hypotension, polyuria
  • Contraindications: hypovolemic hyponatremia, use with CYP3A4 inhibitor
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25
Oxytocin
Induces uterine contractions (alters ion currents across smooth muscle cell membranes), maintains labor, enhances cervical dilation, elicits milk ejection Uses: - Induce, support labor in early vaginal delivery - Low dose: contraction of uterus (increase force, frequency) - High dose: prolonged contractions of uterus, decreases BP causing reflex tachycardia - Nasal spray: induce lactation post-partum
26
Methylergonovine
Rapid, prolonged control of post-partum uterine hemorrhage | - Oral administration
27
Prostoglandins: - Gemeprost (PGE1) - Dinoprostone (PGE2) - Carboprost (PGF2alpha)
Administered injection, intra-amniotically or intravaginally Uses: - Low dose= induces, reinforces labor - High dose= control post-partum bleeding, induce 1st/2nd trimester abortions Adverse effects: diarrhea, hyperthermia, bronchoconstriction
28
Ritodrine
Beta-2 selective agonist: relaxes pregnant uterus to prevent/delay premature parturition - Oral administration - Adverse effects: skeletal muscle tremor, tachycardia - Contraindications: maternal cardiac disease, HTN (pregnancy-induced), uncontrolled DM, hyperthyroidism, hypovolemia, multiple gestation
29
Terbutaline
Beta-2 selective agonist: relaxes pregnant uterus to prevent/delay premature parturition - Oral administration - Adverse effects: skeletal muscle tremor, tachycardia - Contraindications: maternal cardiac disease, HTN (pregnancy-induced), uncontrolled DM, hyperthyroidism, hypovolemia, multiple gestation
30
Magnesium sulfate
Prevents/delays premature parturition (tocolytic)
31
Meds for acromegaly
Pegvisomant (GH receptor antagonist) | Octreotide (somatostatin analogue- inhibits GH release)
32
Meds for dwarfism
Somatotropin (bGH) Somatrem, somatropin (HGH) Mecasermin (IGF-1 recombinant)
33
Meds for prolactinemia
Bromocriptin, cabergoline (dopamine agonists)
34
Diabetes insipidus meds
Central: Vasopressins Nephrogenic: NSAIDs
35
Stimulation of uterine contractions
Prostaglandins (gemeprost, dinoprostone, carboprost) | Oxytocin
36
Inhibition of uterine contractions (tocolytics)
Terbutaline, ritodrine= beta-2 selective agonists | Magnesium sulfate
37
Synthetic TH
Used in treatment of hypothyroidism - Synthetic T4 best absorbed in duodenum, ileum (80%) - Synthetic T3 has 95% absorbtion - Absorption decreased by food, iron, aluminum-containing antacids, sucralfate, calcium preparations - Metabolic clearance increased in drugs inducing liver metabolsim (rifampin, phenobarbital, carbamasepine, phenytoin)
38
Levothyroxine
L-T4 supplement (drug of choice for hypothyroidism Takes longer to activate than T3 supplements (longer to take effect, fewer side effects) Brands: Synthroid, Levoxyl, Unithroid, Levothroid
39
Liothyronine
T3 supplement: cytomel
40
Liothrix
T4/T3 supplement: | Thyrolar
41
Dessicated thyroid
Armour thyroid: combination of types of thyroid ("complete replacement"- not recommended)
42
Methimazole (MMI)
Thionamide: inhibit TPO, block iodine organification. Do NOT block iodide uptake by gland More potent than Propylthioruacyl (PTU) - Readily crosses placenta Dose: 1 time a day Used in treatment of hyperthyroidism; *preferred treatment in MOST cases of hyperthyroidism* Side effects: - 3-12% patients: maculopapular rash, GI - Rare: vasculitis, arthralgia, lupus, liver issues, lymphadenopathy - DANGER: agranulocytosis= neutrophil count < 500 mL (infrequent but fatal- can't fight off infections)
43
Propylothiouracyl (PTU)
Thionamide: inhibit TPO, block iodine organification. *Inhibits conversion of T4 to T3 (unlike methimazole). Do NOT block iodide uptake by gland * Less potent than methimazole* - Given in first trimester pregnancy to avoid harm to fetus (see what happens) Dose: 3 times a day Used in treatment of hyperthyroidism: preferred treatment in pregnancy and Thyroid storm (toxic state) to lower T4-T3 conversion (prevents metabolic conversion) Side effects: - 3-12% patients: maculopapular rash, GI - Rare: vasculitis, arthralgia, lupus, liver issues, lymphadenopathy - DANGER: agranulocytosis= neutrophil count < 500 mL (infrequent but fatal- can't fight off infections)
44
Iodides
Pharmacologic dose inhibits release of TH (inhibits TBG proteolysis?). - Rapidly improves thyrotoxic storm (2-7 days). - Decreases vascularity, size, fragility of hyperplastic gland for pre-operative preparation Side effects: skin rash Dosing: potassium iodide solution
45
Iodinated contrast media
Inhibit conversion of T4 to T3; inhibits release of thyroid hormone Uses: thyroid storm treatment Adverse effects: rare allergic reaction to contrast media
46
Radioactive iodine
I-131= treatment of thyrotoxicosis; destroys thyroid parenchyma--> can lead to HYPOthyroidism - readily incorporated into thyroid follicles Safe: no genetic damage, no leukemia, no neoplasia (v. low dose) Caution: avoid in pregnancy or nursing (can kill fetal/infant thyroid)
47
Beta-blockers for thyroid
Given to treat SYMPTOMS of hyperthyroidism: - Palpitations - Anxiety
48
Caclium supplementation: adverse reactions
``` Major: - Constipation - Nausea - Abdominal pain - Milk alkali syndrome (hypercalcemia, metabolic alkalosis, renal insufficiency) Hypophosphatemia ```
49
Calcium supplementation: Drug/food interactions
- Calcium channel blockers - LEVOTHYROXINE - Antibiotics, atenolol, rion - Thiazide diuretics - Potentiate digoxin toxicity
50
Pharmacokinetics of calcium supplementation
- Calcium carbonate absorption better taken with meals (ACIDIC environment) - Calcium citrate absorbed in fasting state (best in older patients, patients with achlorhydria)
51
Indications for IV calcium
Symptomatic hypocalcemia (serum calcium < 7mg/dL) - Paresthesias - Tetany - Hypotension - Seizures - Chvostek's - Trousseau's - Bradycardia - Prolongation of QT interval
52
Bisphosphanates: MOA
- Inhibit osteoclast bone resorption: attach to bone surfaces undergoing active resorption--> impair ruffled border formation in osteoclast - Decrease osteoclast cell number - Increase BMD, decrease fracture risk
53
Bisphosphanates: PK
Poorly absorbed from GI tract: best on empty stomach | - t1/2= up to 10 years
54
Bisphosphanates: Adverse effects/ contraindications
- GI (abdominal pain, esophageal erosions) - Hypocalcemia (Vit D or Ca deficiency increases risk) - Ocular - Musculoskeletal pain - Osteonecrosis of jaw Contraindications: hypocalcemia, abnormalities of esophagus
55
Clinical use of Bisphosphanates
Oral: Alendronate, risedronate= treat osteoporosis, decrease fracture rates IV: Zoledronic acid= treats hypercalcemia of malignancy, osteoporosis (once yearly infusion), decrease fractures * Monitor creatinine (renal function) prior to each dose
56
Calcitonin
Produced by parafollicular cells surrounding thyroid follicle cells- inhibits osteoclasts, stimulates osteoblasts, increases calcium and phosphate excretion Preparations: Salmon-derived injectable (severe hypercalcemia tx) or inhaled (no effect on calcium- very weak effects on BMD, slight reductions in fractures)
57
Estrogen therapy for Osteoporosis
NOT recommended first-line agent (due to increased risks of CV events)
58
Raloxifine
Selective Estrogen Receptor Modulator (SERM) - Reduces risk of spine fractures- more preventive than therapeutic for fracture patients - Can increase risk of DVT
59
Teraparatide
MOA: PTH--> stimulates osteoblasts, reabsorption of calcium Paradox: PULSATILE PTH= anabolic, stimulates osteoblasts (vs constant PTH= osteoclast activity increased) Uses: most effective osteoporosis treatment Dosing/adminstration= subcutaneous injection Candidates: - Severe osteoporosis (-3.5 or less) - Osteoporosis (-2.5 or less) + fragility fracture - Failure of oral bisphosphanates Adverse reactions: usually due to injection, can't use for >2 years due to osteosarcoma risk
60
Denosumab
Human monoclonal antibody binds to RANK-L MOA: Blocks/interferes with TNF ligand that binds to receptors on pre-osteoclasts--> maturation of osteoclast (Blocks osteoclast maturation, thus bone resorption) - Adverse effects: musculoskeletal pain, eczema, cellulitis, hypocalcemia - - Slight increase in risk of infection due to RANK-L effects on immune function Dosing: subcutaneous injection every 6 months
61
Calcimimetics
- Allosterically increases sensitivity of CaSR in parathyroid gland to calcium - use in dialysis population - hyperparathyroidism without possible surgery
62
Vitamin D supplementation
MOA: 1,25-OH D binds to DNA in intestinal mucosa, bone, kidney tubule cells--> increases intestinal calcium, phosphate absorption - Amplifies action of PTH on bone - Inhibits PTH transcription in chief cells in parathyroid gland PK: easier to absorb than calcium. taken as ergocalciferol (D2) or cholecalciferol (D3- may increase serum 25OH D better than ergo) Adverse reactions: intoxication--> symptoms of hypercalcemia * Assess Vit D status by measuring 25OH-D
63
Calcitriol
Synthetic vitamin D: regulates Ca absorption from GI tract Uses: most active form of VitD to stimulate Ca absorption--> indicated for hypocalcemia, hypoparathyroidism-induced hypocalcemia
64
Glucocorticoids: indications
Endocrine use: diagnosis and cause of Cushing's syndrome; treat adrenal insufficiency, congenital adrenal hyperplasia Non-endocrine use: autoimmune disease, allergies, organ transplant, cancers, derm diseases, respiratory diseases, ophthalmic conditions, GI, nervous system (MS) * All topical, inhaled glucocorticoids absorbed to some extent- can also cause disturbances in hypo-pit-adrenal axis (suppression, Cushing's) - intertriginous areas>> forehead > scalp > face > forearm
65
Glucocorticoids: AE
1. Suppression of Hyp-pit-ad axis - Likely: > 20 mg prednisone/day for > 3 weeks; bedtime evening dose for > 3 weeks; "Cushingoid appearance" - Unlikely: < 3 weeks (any dose); alternate day dosing * avoid adrenal suppression by tapering doses (huge loading dose, taper off) or alternate day administration 2. Cushing's 3. Other: - Fat shifts - hyperglycemia (diabetes) - Osteoporosis - Muscle wasting - Psychosis - Electrolyte imbalance--> edema
66
Mineralocorticoids
Aldosterone (+ progesterone, deoxycorticosterone)--> sodium retention - Aldosterone upregulates Na and K channels: dumps K, resorbs Na
67
Fludrocortisone
Replacement therapy in primary adrenocortical insufficiency MOA: acts like aldosterone (on distal tubules) AEs: hypokalemia, HTN (increased electrolytes), edema Monitoring: orthostatic hypotension measurements, pulse, edema, serum K, plasma renin
68
DHEA-S
``` Adrenal androgen (converted from DHEA) - Can be used as androgen replacement therapy in WOMEN to help with libido (doesn't really help in men) ```
69
Mitotane
Adrenocorticolytic drug for ADRENAL CARCINOMA - medical adrenalectomy AE: N/V, anorexia, diarrhea, rash, gynecomastia, ataxia, arthralgias, leukopenia, hypercholesterolemia, hepatotoxicity
70
Ketoconazole
Most common agent used in treatment of Cushing's disease (pituitary, ectopic) - Given much higher doses than for fungal infections - Inhibits first step in cortisol biosynthesis and blocks conversion of 11-deoxycortisol to cortisol - Inhibits ACTH by impairing corticotroph adenylate cyclase activation AEs: headache, sedation, N/V, gynecomastia, decreased libido/impotence (inhibit testosterone), hepatotoxicity * monitor urine cortisol to adjust doses
71
Spironolactone
Aldosterone receptor antagonist for non-surgical patients - Progesterone and androgen receptor antagonist--> breast tenderness/menstrual irregularities, impotence, decreased libido, gynecomastoa
72
Eplerenone
Mineralocorticoid receptor antagonist (selective) - Doesn't bind androgen/progesterone receptors like spironolactone (fewer AEs) - More expensive
73
Miglitol
Alpha-glucosidase inhibitors MOA: inhibit upper GI enzymes that convert complex polysaccharide carbs into monosaccharides (slow absorption of glucose, slower rise in postprandial blood glucose Side effects: GI (GAS!) Clinical use: only lowers A1C 0.5%, dosed 3 times/day, low hypoglycemia risk, RARELY USED due to weak glucose lowering effects plus bad side effects
74
Pioglitazone (Actos)
Thiazolidinediones MOA: increase insulin sensitivity by stimulating PPAR gamma: - Promotes differentiation of small, metabolically active adipocytes - Alters level of secretory products (reduces TNF and FFA) - Raises adiponectin - Alters adipose tissue distribution (shifts visceral fat to subcutaneous distribution) Leads to improved insulin action, glucose metabolism, vascular function - Rosiglitazone associated with increased risk of ischmic cardiac events--> restricted use - Full clinical effect is slow (2-4 moths) due to alterations in adipocytes/fat distribution - Won't cause hypoglycemia PK: liver metabolism; biologic half life= hours, pharmacologic= months Side effects: peripheral edema (4-6%); weight gain (2-3 kg over 1 year); osteoporosis; hepatotoxicity (rare); macular edema (rare) Clinical use: lower A1c .5-1.4% (small glucose lower effects)
75
Nateglinide
Meglitinides | Slightly different structure, receptor than sulfonylureas, but same MOA. Shorter half life
76
Liraglutide
MOA: synthetic version of Gila monster salivary protein; binds to GLP-1 receptors on beta cells--> stimulates insulin secretion, inhibits glucagon, slows gastric emptying, causes early satiety PK: minimal systemic metabolism; proteolytic degradation; exenatide t1/2= 2-4 hours, liraglutide 1/2= 13 hours Side effects: Nausea (suppresses appetite), jittery/dizzy, headache, pancreatitis, renal failure (do not use with renal clearance < 30), c-cell tumors (contraindicated in medullary thyroid cancer/MEN-2) Clinical use: decrease in A1c 0.5-1.2%, weight loss (5-10 lbs), exenatide dose with meals (liraglutide dosed 2 times/day)
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