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Clinical Pharmacology Flashcards

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1
Q

Actions of Glucocorticoids

A

Anabolic:

  • in liver (gluconeogenesis)
  • also decrease insulin binding to receptors

Catabolic:

  • in muscle, skin, lymph, adipose, and CT
  • redistribute fat twd truncal obesity

Immune System:
- decrease inflammatory rxn, immunocompetent lymphocytes, antigen processing, and ab production

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2
Q

Preferred drug for cortisone replacement therapy

A

Hydrocortisone

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3
Q

Hydrocortisone

A
  • chemically identical to cortisol produced by adrenal glands.
  • Short acting, PO/IV/IM/Topical
  • weak mineralocorticoid effects
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4
Q

Which cortisone derivative = the drug of choice for maintenance therapy of severe asthma

A

Prednisone

- PO, intermediate acting

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5
Q

Which cortisone derivative = the DOC for tx of ACUTE asthmatic attacks (IV)

A

Prednisolone

- IV, intermediate acting

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6
Q

Which cortisone derivative can be used to reduce elevated intracranial pressure

A

dexamethasone

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7
Q

dexamethasone suppression test

A

examines whether the hypothalamus/pituitary can be suppressed by glucoorticoids

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8
Q

which cortisone derivative = the only mineralocorticoid replacement available

A

fludricortisone

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9
Q

Drugs used to Treat Hyperthyroidism (3)

A
  1. Methimazole
  2. Propylthiouracil (PTU)
  3. Iodine/Iodide
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10
Q

Methimazole MOA

A

inhibits transformation of inorganic iodine to organic iodine (thyroxine can’t be formed w/o organic iodine)

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11
Q

SE Methimazole

A
  • temporary hypothyroidism

- agranulocytosis

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12
Q

Propylthiouracil (PTU) MOA

A

blocks conversion of T4 to T3 in tissues (+ the same other MOA of methimazol)
*also same SE’s

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13
Q

Iodine/Iodide for Tx of Hyperthyroidism - MOA

A

inhibits release of thyroxine from thyroid gland

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14
Q

weakness of iodine/iodide

A

only useful for 2 weeks (then thyroid gland adapts and resumes thyroxine secretion)

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15
Q

which anti-hyperthyroidism drug is used for more rapid relief in severely ill pts

A

iodine/iodide

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16
Q

Which drug can be used to relieve symptoms of hyperthyroidism

A

propanolol

b-adrenergic receptor antagonist –> suppresses tachycardia and other catecholamine effects

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17
Q

Drugs used to tx Hypothyroidism (3)

A
  1. Levothyroxine (T4) - e.g., Synthroid
  2. Liothyronine (T3)
  3. Liotrix (T4 and 3) - e.g., Euthyroid
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18
Q

Levothyroxine MOA

A
  • replaces normal serum levels of T4 and T3 (T4 is converted into T3 by deiodination in the periphery)
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19
Q

Drug of choice for hypothyroidism

A

levothyroxine

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20
Q

Used in hypothyroid patients who have difficulty absorbing levothyroxine

A

liothyronine (T3)

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21
Q

Used when conversion of T4 to T3 is abnormally low

A

Liotrix (T4 and T3)

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22
Q

Actions of insulin (on muscle, liver, and adipose)

A

Muscle:

  • increase glucose transport into cell
  • glycogenesis
  • increase protein and triglyceride synthesis

Liver:

  • increase glucose transport into cell
  • glycogenesis
  • increase glucose utilization in Krebs cycle
  • increase protein synthesis

Adipose:

  • increase glucose transport into cell
  • glycogenesis
  • incr. triglyceride synthesis
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23
Q

Trade name for Regular Insulin

A
  • Humulin R

- Novolin R

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24
Q

Trade name for Lispro Insulin

A

Humalog

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25
Trade name for Glargine
Lantus
26
Trade name for Metformin
Glucophage
27
Trade name for Rosiglitazone
Avandia
28
Trade name for Acarbose
Actos
29
Examples of Sulfonylureas
- Glipizide - Glyburide - Glimepiride
30
Sulfonylurea MOA
- insulin secretagogue: close K+ channels in beta cells of pancreas --> increase insulin release - increases the sensitivity of tissues to the actions of insulin
31
SE of sulfonylureas
hypoglycemia | weight gain
32
MOA Metformin
- reduces intestinal uptake and hepatic production of glucose (also reduces renal gluconeogenesis) - increases sensitivity of tissues to insulin
33
SE of Metformin
- lactic acidosis (can be fatal) - most common = GI side effects *note : does NOT cause hypoglycemia
34
Alpha-glucosidase inhibitors (2)
- Miglitol | - Acarbose
35
MOA alpha-glucosidase inhibitors
- inhibit intestinal alpha-glucosidases (reduce conversion of starch and disaccharides to monosaccharides) and thus slows carb digestion resulting in lower serum glucose after meals ** decreases post-prandial hyperglycemia
36
SE of alpha-glucosidase inhibitors
- flatulence - diarrhea - abdominal pain
37
Thiazolidinediones (2)
- Rosiglitazone | - Pioglitazone
38
MOA Thiazolidinediones
- regulate gene expression by binding to PPAR-gamma (and alpha for pioglitazone) - enhance response of target cells (e.g., liver and muscle) to endogenous insulin, perhaps by activating nuclear receptors that increase the transcription of glucose control genes
39
what do you need to check with glitazones/ what are the SE's
- monitor LFT's - and d/c if LFT > 3x normal SE's: - fluid retention, edema, macular edema - anemia - weight gain - bone fractures in women ** cannot use in CHF or hepatic disease
40
Repaglinide MOA
- insulin secretagogue (similar to sulfonylureas) - blocks potassium channels in pancreatic beta cells --> leads to depolarization, calcium influx, and ultimately insulin secretion ** oral w/ very fast onset and shorter duration (1/2 to 1/3 the time of sulfonylureas)
41
Which DM drugs require functioning beta cells of pancreas?
- sulfonylureas - glitazones (rosi and pio) - repaglinide
42
Examples of Rapid acting Insulin
- Lispro | - Aspart
43
Examples of Short acting insulin
Regular Insulin
44
Examples of Intermediate acting Insulin
NPH
45
Examples of long acting insulin
- Determir | - Glargine
46
Neg SE's of Insulin
- hypoglycemia - weight gain - lipodystrophy (rare)
47
When is Metformin CI?
if impaired renal/hepatic function
48
Incretin based DM drugs
1. Exenatide (IV) | 2. Sitagliptin (PO)
49
Amylin Analog DM drug
Pramlintide
50
MOA Incretin-based drugs
1. Exenatide (analog of GLP-1: binds to GLP-1 receptors) 2. Sitagliptin (DPP-4 inihibitor: blocks degradation of GLP-1; raises circulating levels of GLP-1) ** both reduce post-meal glucose excursions: increase glucose-mediated insulin release, lowers glucagon levels, slows gastric emptying, and decreases appetite
51
MOA Pramlintide
- analog of amylin: binds to amylin receptors and reduces post-meal glucose excursions; lowers glucagon levels; slows gastric emptying; decreases appetite
52
SE Exenatide
- N/V/H - anorexia, wt loss - PANCREATITIS
53
SE Sitagliptin
- Rhinitis | - URI's, rare allergic rxns
54
SE Pramlintide
- hypoglycemia | - headache, nausea, anorexia
55
Subclasses of Drugs used in Asthma
- Beta agonists (mostly B2) - Corticosteroids (Inhaled or Systemic) - Stabilizers of Mast/Other Cells - Methylxanthines - Leukotriene Antagonists - IgE antibody
56
Beta Agonists used for asthma
1. Albuterol (B2 agonist) - similar: metaproterenol, terbutaline 2. Salmeterol (B2 agonist) - similar: formeterol 3. Epinephrine (Non-selective alpha and beta agonist) 4. Isoproterenol (B1 and B2 agonist)
57
Drug of choice for acute asthmatic bronchospasm
Albuterol (--> prompt bronchodilation lasting several hours)
58
Which Beta agonist is used mostly for asthma prophylaxis
salmeterol *(slow onset, potentiates corticosteroid effect)
59
Most common use for Epinephrine
anaphylaxis *rarely used for asthma b/c B2 agonists = preferred
60
Why isn't isoproterenol preferred for asthma?
b/c despite bronchodilation, it is has powerful CV effects due to fact it is B1 and B2 agonist
61
Which corticosteroids tend to be used for asthma?
1. Fluticasone 2. Prednisone ** both mediate inflammatory response via gene expression and can be used in both acute and prophylactic circumstances
62
Examples of mast cell stabilizers for asthma
1. Cromolyn | 2. Nedocromil
63
How does Cromolyn work?
alters function of delayed chloride channels -- inhibits inflammatory cell activation so as to prevent acute bronchospasm
64
Which asthma drug is not absorbed, therefore reducing most toxicities
cromolyn (only aerosol)
65
Theophylline MOA and use
- causes bronchodilation, cardiac stimulation, and increased skeletal muscle strength - used for asthma and COPD
66
Which drugs used mostly for prophylaxis of asthma, especially in children and ASA-induced asthma?
Leukotriene antagonists: montelukast and zafirlukast
67
Which drug is a humanized IgE antibody that reduces circulating IgE and is used to reduce frequency of asthma exacerbations
Omalizumab (IV)
68
Trade name for Acetaminophen
Tylenol
69
Actions of Acetaminophen
- analgesic - anti-pyretic NO ANTI-INFLAMM EFFECTS!
70
Which drug is preferred over aspirin in children b/c it is less likely to cause Reye's Syndrome
Tylenol
71
OD of Acetaminophen may cause:
- severe hepatic necrosis --> coma/death
72
MOA/Actions of NSAIDS
- inhibit cyclooxygenase (COX), an enzyme required for synthesis of prostaglandins - analgesic - anti-inflammatory - anti-pyretic ** prevents platelet aggregation (except COX-2)
73
NSAIDS contraindicated in what pts
- bleeding disorders | - peptic ulcer dz
74
SE NSAIDS
- GI upset (take with food) | - bleeding/ increased risk of bleeding with anticoagulants

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