(anti-hyperlipidemia & anti-inflammatory drugs)Ch 21 & 41 WEEK 13---Q = 23 Flashcards

1
Q

ANTIhyperlipidemia–Chapter 21

Hyperlipidemias are a complex diseases due to:
• PRIMARY factors (such as: _________ or environmental factors..,
• and SECONDARY factors due to _______ ______ (such as: diabetes, alcoholism, hypothyroidism or biliary cirrhosis)
• all these factors lead to →↑ LDL and ↓ HDL

A

genetic

metabolic diseases

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2
Q

ANTIhyperlipidemia–Chapter 21

Drugs that ↓serum lipoprotein level

  1. Niacin (Nicotinic acid, Nicobid)
    — Action: it is a water-soluble vitamin, that inhibits __________ in adipose tissue → ↓ liver triglyceride
    → ↓ VLDL & LDL formation.

Uses: _______ ___________ _______

Side effects: _____ _______, an itching (pruritis), some nausea & abdominal pain., may be gout

A

lipolysis

high cholesterol level

skin flushing

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3
Q

ANTIhyperlipidemia–Chapter 21

Drugs that ↓serum lipoprotein level

  1. The FIBRATES (Clofibrate {Atromide-S})
    Actions: Clofibrate stimulates ______ ________ that breakdown the triglyceride into free fatty acid and
    remove the particles from the plasma.

Uses: in _________________

Side effects:

  1. mild GI disturbance
  2. ↑ biliary cholesterol → _______ _______
  3. Myositis

Drug interaction: it ↑anticoagulants (such as: cumarin) activity

A

lipoprotein lipase

hypertriglyceridemia

gall stones

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4
Q

ANTIhyperlipidemia–Chapter 21

Drugs that ↓serum lipoprotein level

  1. Bile acid binding resins (cholestyramine {Questran}, colestipol {Colestid})

—Actions: cholestyramine, _____ bile ACID and bile SALT in the small intestine (called resin/bile acid complex), which is excreted in the feces.

 Uses: _______________

Side effects:

  1. ___ ________: such as, constipation, nausea & flatulence.
  2. Impaired absorption of FAT-soluble vitamins (A, D, K & E), also folic acid and vitamin C are reduced.

Drug interactions: cholestyramine, _________ with the
intestinal absorption of many drugs, such as: tetracycline,
phenobarbital, warfarin, aspirin, & thiazide diuretics.

A

binds

hyperlipidemia

GI disturbances

interferes

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5
Q

ANTIhyperlipidemia–Chapter 21

Drugs that ↓serum lipoprotein level

***** Probucol (Lorelco) (NOT IN BOOK)

Actions: unknown, but probucol inhibits the oxidation
of cholesterol, to prevent ___________ formation.

Uses: in hyperlipidemia, (unfavor now because it → ↓
HDL as will as LDL).

A

atherosclerosis

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6
Q

ANTIhyperlipidemia–Chapter 21

Drugs that ↓serum lipoprotein level

  1. Cholesterol absorption inhibitors = Ezetimibe (Zetia):
    Lower LDL cholesterol 17%, TG 6%
    Avoid use in ____________ diseases
A

hepatic

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7
Q

ANTIhyperlipidemia–Chapter 21

Drugs that ↓serum lipoprotein level

  1. HMG-CoA reductase inhibitors: lovastatin (Mevacor), simvastatin (ZOCOR)

Actions: these drugs inhibit the rate-limiting step in _________ _________ by inhibiting HMG-CoA
(hydroxymethylglutaryl- coenzyme A) reductase.

Uses: in all types of _______________

Side effects: (VERY IMPORTANT!!)

  1. Abnormalities in ______ function, →↑ serum transaminases (SGOT, or SGPT).
  2. It causes myopathy and rhabdomyolysis (disintegration or dissolution of ___________)

Drug interactions: it causes →↑ cumarin levels.

Contraindications: in PREGNANCY & NURSING mothers

A

cholesterol synthesis

hyperlipidemia

liver

muscles

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8
Q

Anti-inflammatory drugs—chapter 41

Inflammation:
Cardinal signs of inflammation are:
—Calor, rubor, tumor, dolor, loss of function

Chemical mediators of inflammation are:
__________, histamine, ________, kinin, interleukin-1,
neutrophil,

A

prostaglandins

bradykinin

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9
Q

Anti-inflammatory drugs—chapter 41

Prostaglandin synthesis

1—-prostaglandins are one of the chemical mediators that are released in _______AND___________ reactions.

2—PGs stimulate TXA2 for platelets aggregation

A

allergy and inflammatory

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10
Q

Anti-inflammatory drugs—chapter 41

NSAIDs
1. Aspirin–part 1

Actions:
aspirin is an acetyl-salicylic acid, as antipyretic (fever), anti-inflammatory by decreasing the PGs synthesis (inhibits___________), and analgesic (pain) by depress the pain stimuli.

Respiratory:

  1. ⇑ alveolar ventilation
  2. Higher doses ⇒ hyperventilation and respiratory __________
A

cyclooxygenase

alkalosis.

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11
Q

Anti-inflammatory drugs—chapter 41

  1. Aspirin—part 2

—Blood: as anti-coagulant, inhibits platelet aggregation ⇒ prolonged _________ ________

—-GI tract: ⇑ gastric secretion ⇒ gastric distress, __________ and/or hemorrhage.

—Kidney: DECREASES PGs synthesis ⇒result in retention of Na+ & water ⇒ ______ & hyperkalemia, aspirin does NOT cause interstitial nephritis such as the rest of NSAIDs.

A

bleeding time.

ulceration

edema

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12
Q

Anti-inflammatory drugs—chapter 41

  1. Aspirin—part 3

Uses:
a. anti-pyretic, to relief fever (except, contraindicated in _______syndrome which is developed by using aspirin with chicken pox or influenza = flu)
b. analgesic, and ___-_________, in rheumatoid
arthritis, rheumatic fever, gout (high dose).
c. to ⇓ transient ischemic attack, unstable ANGINA
and coronary artery thrombosis.

• Side effects:
1. GI: nausea, vomiting, gastritis, __ __________, which can be treated by Misoprostol (Cytotec) to enhance mucosal resistance
2. Blood: a prolonged bleeding time
3. Allergy
4. Respiration: respiratory depression, respiratory and
metabolic acidosis, in toxic levels (resp. paralysis)
5. Reye’s syndrome: hepatitis with cerebral edema,
6. Drug interactions:

A

Reye’s

anti-inflammatory

GI bleeding

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13
Q

Anti-inflammatory drugs—chapter 41

  1. Aspirin–part 4 of 4

Toxicity:

a. MILD form (salicylism): _______,vomiting, hyperventilation, headache, dizziness, tinnitus and mental confusion
b. SEVERE form: CNS disturbance, hallucinations, delirium, convulsions, coma, acidosis, and _______

Treatment of intoxication:
gastric lavage, IV fluids, hemodialysis

A

nausea

death

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14
Q

Anti-inflammatory drugs—chapter 41

  1. Ibuprofen (motrin) & Naproxen (anaprox)

Actions: ___________________, analgesic, & antipyretic
more effective analgesic than ______ both Ibuprofen & Naproxen are potent reversible cyclooxygenase inhibitors.

Uses: inflammation, fever, pain

Side effects:
1–GI disturbance (bleeding, gastritis, ulcer),
2–prolonged bleeding time
3–______ (interstitial nephritis).

A

anti-inflammatory

aspirin

kidney

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15
Q

Anti-inflammatory drugs—chapter 41

NSAIDs #1
3. INDOmethacin

Actions & uses:

  1. More potent anti-inflammatory agent in _______ arthritis, ankylosing spondylitis, and acute gouty arthritis.
  2. Antipyretic
  3. Analgesic

Side effects:

  1. GI complaints: (_______, bleeding, pain, diarrhea, anorexia),
  2. CNS: (frontal headache, dizziness, vertigo, mental confusion)
  3. Blood reactions: _________, and thrombocytopenia
A

rheumatoid

ulcers

neutropenia

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16
Q

Anti-inflammatory drugs—chapter 41

NSAIDs
4. Phenylbutazone (not mentioned in 4th ed.)

Actions: the most powerful anti-inflammatory effects, but weak _________ and __________
Uses: in short term (up to 1 week) in acute gout & acute rheumatoid arthritis

Side effects:

  1. The most serious effect is agranulocytosis and aplastic anemia
  2. ________ __________, nausea, vomiting..
A

analgesic & antipyretic.

Peptic ulcer

17
Q

Anti-inflammatory drugs—chapter 41

NON-narcotic analgesics
1—-acetaminophen (tylenol)

Actions: acetaminophen act by inhibiting _________
synthesis in the CNS (STRONG analgesic and anti-pyretic but WEAK _____________) no effects on platelet function or blood clotting.

Uses:

  • —substitute for aspirin, as antipyretic or analgesic,
  • —-acetaminophen is conjugated in the liver ⇒ to form inactive glucuronidated metabolites,
  • —– but it is hydroxylated ⇒ to form a toxic metabolite ⇒ damage the liver.

Side effects:

  1. Skin rash & allergy
  2. Renal tubular necrosis-kidney
  3. Hypoglycemic coma
  4. _________ _______ (dose >13 gm)
    * ** Antidote: N-acetylcysteine
A

prostaglandin

anti-inflammatory

Liver damage

18
Q

Anti-inflammatory drugs—chapter 41

Slow acting, anti-inflammatory agents
a. Gold salts

Actions: Gold salts (gold sodium thiomalate), is believed
that are taken by macrophages ⇒ to suppress
phagocytosis & lysosomal enzyme activity for any more
bone destruction. Can’t REPAIR the injury but PREVENT it

Uses: ____________ ________ & any advanced arthritis

Side effects:

  1. ______________
  2. proteinurea
  3. Diarrhea
  4. Thrombocytopenia
  5. Encephalitis, hepatitis, neuritis.

***__________: for SEVERE rheumatoid arthritis with NO
response to other treatment.

A

rheumatoid arthritis

dermatitis

Methotrexate

19
Q

Anti-inflammatory drugs—chapter 41

Drugs used in the treatment of GOUT

Gout is a metabolic disorder characterized by high level of uric acid in the blood.
1—-_________ ⇒ deposition of sodium urate crystals in the kidney & joints ⇒ initiate kidney stones & joint
inflammation
2—_______ ______ is the end product of purine metabolism.
3—ACUTE GOUT = treated by ________ AND indomethacin (NSAIDs)
4—CHRONIC GOUT treated by ____________/or probenecid

A

hyperurecemia

Sodium urate

colchicine

allopurinol

20
Q

Drugs used in the treatment of GOUT

Anti-inflammatory drugs—chapter 41

_______________ AND _____________

A

Colchicine & allopurinol

21
Q

Anti-inflammatory drugs—chapter 41

Drugs used in the treatment of GOUT

A. Colchicine

Actions:
1. Colchicine binds to tubulin (a microtubular protein), which causes the depolymerization ⇒ prevent the
mobility of granulocytes.
2. inhibits the synthesis and release of leukotrienes
(–lipooxygenase)

Uses: in ACUTE gout (to relieve pain within ____ hours)

Side effects:
1. GI problems: nausea, vomiting, abdominal pain AND diarrhea
2. In CHRONIC use: ⇒ myopathy, agranulocytosis, aplastic anemia AND alopecia
(regular dose in adult:0.5 mg every hour)
—- a fatal dose of colchicine can be as little as __ mg in ____ hours

A

12

8

24

22
Q

Anti-inflammatory drugs—chapter 41

Drugs used in the treatment of GOUT

B. Allopurinol

Actions: allopurinol reduces the production of uric acid by
inhibiting _________ __________, (which converts xanthine or hypoxanthine to uric acid)

Uses: in CHRONIC gout to treat hyperurecemia.

Side effects:

  1. Allergy (_______ ____= MC side effect)
  2. Acute attacks of gout during the first weeks of therapy (should add colchicine)
  3. GI problems: nausea & diarrhea
A

xanthine oxidase

skin rashes