(anti-hyperlipidemia & anti-inflammatory drugs)Ch 21 & 41 WEEK 13---Q = 23 Flashcards
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
genetic
metabolic diseases
ANTIhyperlipidemia–Chapter 21
Drugs that ↓serum lipoprotein level
- 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
lipolysis
high cholesterol level
skin flushing
ANTIhyperlipidemia–Chapter 21
Drugs that ↓serum lipoprotein level
- 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:
- mild GI disturbance
- ↑ biliary cholesterol → _______ _______
- Myositis
Drug interaction: it ↑anticoagulants (such as: cumarin) activity
lipoprotein lipase
hypertriglyceridemia
gall stones
ANTIhyperlipidemia–Chapter 21
Drugs that ↓serum lipoprotein level
- 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:
- ___ ________: such as, constipation, nausea & flatulence.
- 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.
binds
hyperlipidemia
GI disturbances
interferes
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).
atherosclerosis
ANTIhyperlipidemia–Chapter 21
Drugs that ↓serum lipoprotein level
- Cholesterol absorption inhibitors = Ezetimibe (Zetia):
Lower LDL cholesterol 17%, TG 6%
Avoid use in ____________ diseases
hepatic
ANTIhyperlipidemia–Chapter 21
Drugs that ↓serum lipoprotein level
- 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!!)
- Abnormalities in ______ function, →↑ serum transaminases (SGOT, or SGPT).
- It causes myopathy and rhabdomyolysis (disintegration or dissolution of ___________)
Drug interactions: it causes →↑ cumarin levels.
Contraindications: in PREGNANCY & NURSING mothers
cholesterol synthesis
hyperlipidemia
liver
muscles
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,
prostaglandins
bradykinin
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
allergy and inflammatory
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:
- ⇑ alveolar ventilation
- Higher doses ⇒ hyperventilation and respiratory __________
cyclooxygenase
alkalosis.
Anti-inflammatory drugs—chapter 41
- 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.
bleeding time.
ulceration
edema
Anti-inflammatory drugs—chapter 41
- 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:
Reye’s
anti-inflammatory
GI bleeding
Anti-inflammatory drugs—chapter 41
- 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
nausea
death
Anti-inflammatory drugs—chapter 41
- 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).
anti-inflammatory
aspirin
kidney
Anti-inflammatory drugs—chapter 41
NSAIDs #1
3. INDOmethacin
Actions & uses:
- More potent anti-inflammatory agent in _______ arthritis, ankylosing spondylitis, and acute gouty arthritis.
- Antipyretic
- Analgesic
Side effects:
- GI complaints: (_______, bleeding, pain, diarrhea, anorexia),
- CNS: (frontal headache, dizziness, vertigo, mental confusion)
- Blood reactions: _________, and thrombocytopenia
rheumatoid
ulcers
neutropenia