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Clinical Pharmacology Flashcards

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
Q

Trade name for Glargine

A

Lantus

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26
Q

Trade name for Metformin

A

Glucophage

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27
Q

Trade name for Rosiglitazone

A

Avandia

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28
Q

Trade name for Acarbose

A

Actos

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29
Q

Examples of Sulfonylureas

A
  • Glipizide
  • Glyburide
  • Glimepiride
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30
Q

Sulfonylurea MOA

A
  • insulin secretagogue: close K+ channels in beta cells of pancreas –> increase insulin release
  • increases the sensitivity of tissues to the actions of insulin
31
Q

SE of sulfonylureas

A

hypoglycemia

weight gain

32
Q

MOA Metformin

A
  • reduces intestinal uptake and hepatic production of glucose (also reduces renal gluconeogenesis)
  • increases sensitivity of tissues to insulin
33
Q

SE of Metformin

A
  • lactic acidosis (can be fatal)
  • most common = GI side effects

*note : does NOT cause hypoglycemia

34
Q

Alpha-glucosidase inhibitors (2)

A
  • Miglitol

- Acarbose

35
Q

MOA alpha-glucosidase inhibitors

A
  • 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
Q

SE of alpha-glucosidase inhibitors

A
  • flatulence
  • diarrhea
  • abdominal pain
37
Q

Thiazolidinediones (2)

A
  • Rosiglitazone

- Pioglitazone

38
Q

MOA Thiazolidinediones

A
  • 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
Q

what do you need to check with glitazones/ what are the SE’s

A
  • 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
Q

Repaglinide MOA

A
  • 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
Q

Which DM drugs require functioning beta cells of pancreas?

A
  • sulfonylureas
  • glitazones (rosi and pio)
  • repaglinide
42
Q

Examples of Rapid acting Insulin

A
  • Lispro

- Aspart

43
Q

Examples of Short acting insulin

A

Regular Insulin

44
Q

Examples of Intermediate acting Insulin

A

NPH

45
Q

Examples of long acting insulin

A
  • Determir

- Glargine

46
Q

Neg SE’s of Insulin

A
  • hypoglycemia
  • weight gain
  • lipodystrophy (rare)
47
Q

When is Metformin CI?

A

if impaired renal/hepatic function

48
Q

Incretin based DM drugs

A
  1. Exenatide (IV)

2. Sitagliptin (PO)

49
Q

Amylin Analog DM drug

A

Pramlintide

50
Q

MOA Incretin-based drugs

A
  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
Q

MOA Pramlintide

A
  • analog of amylin: binds to amylin receptors and reduces post-meal glucose excursions; lowers glucagon levels; slows gastric emptying; decreases appetite
52
Q

SE Exenatide

A
  • N/V/H
  • anorexia, wt loss
  • PANCREATITIS
53
Q

SE Sitagliptin

A
  • Rhinitis

- URI’s, rare allergic rxns

54
Q

SE Pramlintide

A
  • hypoglycemia

- headache, nausea, anorexia

55
Q

Subclasses of Drugs used in Asthma

A
  • Beta agonists (mostly B2)
  • Corticosteroids (Inhaled or Systemic)
  • Stabilizers of Mast/Other Cells
  • Methylxanthines
  • Leukotriene Antagonists
  • IgE antibody
56
Q

Beta Agonists used for asthma

A
  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
Q

Drug of choice for acute asthmatic bronchospasm

A

Albuterol (–> prompt bronchodilation lasting several hours)

58
Q

Which Beta agonist is used mostly for asthma prophylaxis

A

salmeterol

*(slow onset, potentiates corticosteroid effect)

59
Q

Most common use for Epinephrine

A

anaphylaxis

*rarely used for asthma b/c B2 agonists = preferred

60
Q

Why isn’t isoproterenol preferred for asthma?

A

b/c despite bronchodilation, it is has powerful CV effects due to fact it is B1 and B2 agonist

61
Q

Which corticosteroids tend to be used for asthma?

A
  1. Fluticasone
  2. Prednisone

** both mediate inflammatory response via gene expression and can be used in both acute and prophylactic circumstances

62
Q

Examples of mast cell stabilizers for asthma

A
  1. Cromolyn

2. Nedocromil

63
Q

How does Cromolyn work?

A

alters function of delayed chloride channels – inhibits inflammatory cell activation so as to prevent acute bronchospasm

64
Q

Which asthma drug is not absorbed, therefore reducing most toxicities

A

cromolyn (only aerosol)

65
Q

Theophylline MOA and use

A
  • causes bronchodilation, cardiac stimulation, and increased skeletal muscle strength
  • used for asthma and COPD
66
Q

Which drugs used mostly for prophylaxis of asthma, especially in children and ASA-induced asthma?

A

Leukotriene antagonists: montelukast and zafirlukast

67
Q

Which drug is a humanized IgE antibody that reduces circulating IgE and is used to reduce frequency of asthma exacerbations

A

Omalizumab (IV)

68
Q

Trade name for Acetaminophen

A

Tylenol

69
Q

Actions of Acetaminophen

A
  • analgesic
  • anti-pyretic

NO ANTI-INFLAMM EFFECTS!

70
Q

Which drug is preferred over aspirin in children b/c it is less likely to cause Reye’s Syndrome

A

Tylenol

71
Q

OD of Acetaminophen may cause:

A
  • severe hepatic necrosis –> coma/death
72
Q

MOA/Actions of NSAIDS

A
  • inhibit cyclooxygenase (COX), an enzyme required for synthesis of prostaglandins
  • analgesic
  • anti-inflammatory
  • anti-pyretic

** prevents platelet aggregation (except COX-2)

73
Q

NSAIDS contraindicated in what pts

A
  • bleeding disorders

- peptic ulcer dz

74
Q

SE NSAIDS

A
  • GI upset (take with food)

- bleeding/ increased risk of bleeding with anticoagulants

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