(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
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:
- The most serious effect is agranulocytosis and aplastic anemia
- ________ __________, nausea, vomiting..
analgesic & antipyretic.
Peptic ulcer
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:
- Skin rash & allergy
- Renal tubular necrosis-kidney
- Hypoglycemic coma
- _________ _______ (dose >13 gm)
* ** Antidote: N-acetylcysteine
prostaglandin
anti-inflammatory
Liver damage
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:
- ______________
- proteinurea
- Diarrhea
- Thrombocytopenia
- Encephalitis, hepatitis, neuritis.
***__________: for SEVERE rheumatoid arthritis with NO
response to other treatment.
rheumatoid arthritis
dermatitis
Methotrexate
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
hyperurecemia
Sodium urate
colchicine
allopurinol
Drugs used in the treatment of GOUT
Anti-inflammatory drugs—chapter 41
_______________ AND _____________
Colchicine & allopurinol
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
12
8
24
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:
- Allergy (_______ ____= MC side effect)
- Acute attacks of gout during the first weeks of therapy (should add colchicine)
- GI problems: nausea & diarrhea
xanthine oxidase
skin rashes
