Pharmacology 26 & 27 Drugs Affecting Lipid Levels & Urinary Output

Front 1

(P) LOVASTATIN

Back 1

ANTI-HYERLIPIDEMICS --> STATIN

4:
1o & combined
high cholesterol
prevents 2o coronary evnts (MI, stroke)
+off-labels

MECH:
competitively inhibits HMG-CoA reductase (which catalyzes rate-limiting step in cholest. synthesis)
= decrs LDL (-21-40%) & incrs HDL

CONTRAS:
active liver dis (elevated liver func)
Preg cat X

ADVERSES:
- muscle/joint aches
- Rhabdomyolysis (muscle damage: CK levels 10,000 U/L+ or +10x upper limit w/ renal problems)
- elevated heptatic enzymes

- high 1st pass effect (only 5% of PO reaches gen circ)

- best absorbed after a meal

-metabolized w/ CYP 3A4 (= grapefruit juice = inhibitor = more drug in circ = grtr toxicty risk)

- do AST & ALT tests (liver func tests) & baseline CK level B4

Front 2

high serum lipid levels associated with (4)

Back 2

1) hypertension
2) coronary artery disease
3) coronary heart disease
4) other CV disords.

Front 3

cholesterol produced in _____ at rate of _____ mg/day

Back 3

liver

1000mg/day

Front 4

hyperlipidemia 冒isk factor for ___?

Back 4

atherosclerosis ("paste" buildup)

leads to HPN --> MI & stroke

Front 5

normal a high levels of LDL?

Back 5

<100 mg/dL = optimal

>130 mg/dL = high

Front 6

normal and high level for total cholesterol?

Back 6

<200 mg/dL = normal

>230 mg/dL = high

Front 7

normal and low levels for HDL?

Back 7

40-59 mg/dL = optimal

<35 mg/dL = low

Front 8

何hat are the 冒isk factors for metabolic syndrome?

Back 8

hyperlipidemia
insulin resistance
obesity
HTN

Front 9

how can the endothelium of vessels contribute to vascular homeostasis?

Back 9

a well-functioning endothelium has:

vasodilatory
anti-coagulant
anti-inflammatory functions

these are often absent in atherosclerosis

Front 10

何hat is combined hyperlipidemia?

People with this exhibit 何hat?

Back 10

an elevated 均evel 之f more than 1 serum lipid

a 据et lipid profile

Front 11

Why are diabetic patients at increased risk when they have hyperlipidemia?

Back 11

link btwn hyperlipidemia & nephropathy (an atherosclerotic process occurs to mesangial cells in the kidneys b/c cholesterol binds to them)

Front 12

list some of the "therapeutic lifestyle changes" that are recommended 2 reduce LDL levels (8)

Back 12

down:
sat fats
trans fats
cholesterol
fatty acids
weight

up:
phys activity
soluble fiber
plant sterols
plant stanols

Front 13

10% reduction in cholesterol level leads to ______% reduction in risk for CHD?

Back 13

20 - 30%

Front 14

statins pull ___(6)____ down?

Back 14

down:

血lood cholesterol
uptake 之f modified lipoprotiens by vascular cells
CV events
inflammatory response (less C-reactive proteins)
thrombogenicity 之f the 血lood
oxidative stress

Front 15

(P) HYDROCHLOROTHIAZIDE

HTCZ

Back 15

PRODUCE DIURESIS --> THIAZIDE DIURETICS

4:
hypertension

MECH:
limits reabsorption 之f Na+ 中n distal tubule by inhibiting ion pumps

CONTRAS:
Severe renal impairment, anuria, hepatic coma, and hypersensitivity

ADVERSES:
HYPO-kalemia, -natremia, -chloremia, and -calcemia
Orthostatic hypotension

- watch Na intake (get baseline)

- 作ake sure they 可an get to a toilet

- watch 体ody weight changes to 見ee if they're loosing H2O weight

Front 16

(P) FUROSAMIDE

Back 16

DRUGS PRODUCING DIURESIS --> LOOP DIURETICS

4:
peripheral & pulmonary edema
HTN

MECH:
work in the loop of Henle to inhibit re­absorption of sodium
- Highly protein-bound & high-ceiling

CONTRAS:
Anuria
hypokalemia (NOT K-sparing)

ADVERSES:
Electrolyte imbalance, ototoxicity, alteration in glucose levels
Hypovolemia (if OD)

* do not give with digoxin or aminoglycoside

- WATCH CBC, serum electrolyte & uric acid levels

- watch Na intake (get baseline)

Front 17

(P) TRIAMTERINE

Back 17

DRUGS PRODUCING DIURESIS --> K-SPARING DIURETIC

4:
edema
HTN

MECH:
inhibits reuptake of Na in distal tubules - independent of aldosterone
elevates serum uric acid levels

CONTRAS:
Hyperkalemia, renal or liver disease

ADVERSES:
Hyperkalemia, nephrotox, thrombocytopenia, UP liver enzymes, headA, and photosens

- asses for other drugs that increase K levels (also limit K intake)

- give in morning

- intracts w/ AMANTADINE

Front 18

(P) MANNITOL

Back 18

DRUGS PRODUCING DIURESIS --> OSMOTIC DIURETIC

4:
ARF (acute renal failure)
reducing intracranial pressure in cerebral edema
reducing intraocular pressure

MECH:
Increases concentration of molecules in glomerular filtrate = MORE H2O flow in2 tubules & more pee.
- POORLY metabolized

CONTRAS:
Severe renal disease, pulmonary congestion, or active intracranial bleeding

ADVERSES:
Fluid or electrolyte losses, hypOtension, tachycardia

- only given in acute care setting

- don't give > 15% conc.

Front 19

(P) ACETAZOLAMIDE

Back 19

DRUGS PRODUCING DIURESIS --> CARBONIC ANHYDRASE INHIBITORS

4:
chronic open-angle glaucoma

MECH:
Blocks the action of carbonic anhydrase, (needed for active transport of ions across the proximal tubule) --> less H ion secretion, but more Na,K secretion.

Decreases formation of aqueous humor--> less introoccular pressure--> lowers pH of body fluids

CONTRAS:
Kidney & liver disease, adrenocortical insufficiency, COPD, cirrhosis, and closed-angle glaucoma

ADVERSES:
Anorexia, N & C, CNS d's, paresthesia, ataxia, tremor, and tinnitus

- Monitor CBC & platelet counts (Bone marrow suppression can happen...)

Front 20

(P) TOLTERADINE

Back 20

DRUGS PRODUCING DIURESIS --> affect bladder funcion --> ANTICHOLINERGICS

4:
overactive bladder and incontinence

MECH:
Competitive cholinergic muscarinic antagonist

CONTRAS:
Urinary retention, gastric retention, uncontrolled narrow-角ngle glaucoma, or hypersensitivity

ADVERSES:
干ry mouth, constipation, abnormal vision, urinary retention, and xerophthalmia


- Protein bound

Front 21

Statins bring _____(3)____ up/助elp 何hat?

Back 21

助elp:

vascular endothelium
availability 之f nitric oxide (helps endothelium)
vasodilation

-may also prevent Alzheimer's & w/ Tx 之f MS, neuroinflammatory dis, & chronic renal disease

Front 22

Statins are the only class of antilipid drugs shown to____?

also (2)

Back 22

Decrease overall mortality in both 1o and 2o (established CAD) prevention

also:
1) decrease risk of stroke
2) are more effective when used jointly

Front 23

do you need a liver panel b4 giving Pravastatin?

why?

Back 23

no - becasue it is not metabolized by the CYP-450 class of isoenzymes

Front 24

FENOFIBRATE

GEMFIBROZIL

Back 24

ANTIHYPERLIPIDEMICS --> FIBRIC-ACID DERIVATIVES

4:
hyperlipidemia (high cholesterol)
2ND LINE

CONTRAS:
hepatic / renal probs

ADVERSES:
Serious Hepatic & renal Fxs
rhabdomyolysis
hyperglycemia

* sometimes combined with lovastatin if lvls don't come down *

Front 25

NIACIN

Back 25

HYPERLIPIDEMIA --> NICOTINIC ACID

4:
hyperlipidemia
3RD LINE

MECH:
reduces LDL - increases HDL

* dramatic SUBCUTANEOUS FLUSH (sustained release forms - not so bad now) *

Front 26

CHOLESTYRAMINE

Back 26

ANTI=HYPERLIPIDEMICS --> BILA ACID SEQUESTRANTS

4:
hyperlipidemia
4TH LINE

MECH:
Promote oxidation of cholesterol to bile acid (work in GI tract), bind the bile acid and its excreted

* Choleterol serum lvls usually down after 1 month Tx *

* given b4 meal *

Front 27

Diuresis?

Diuretics?

Back 27

ridding body of fluids by inc product of urine - excreting H2O & electrolytes

promote this

Front 28

Diuretics general MECH?

Back 28

block reabsorption of Na+ & promote its excretion

- other E-'s may also be blocked from reabsorption (K+)

Front 29

5 classes of Diuretics?

Back 29

1) Thiazide
2) loop
3) K+ - sparing
4) Osmotic
5) carbonic anhydrase inhibitors

Front 30

which types of diuretics decrease circulating volume?

where does each work?

Back 30

1) Thiazide - (works in distal tubule)
2) loop - (Loop of Henle)
3) K+ sparing - (distal tubule)

Front 31

What do Osmotic diuretics do? (2)

Back 31

1) decrease intraoccular & intracranial pressure

2) Tx or prevent Renal failure

Front 32

Carbonic Anhydrase inhibitor MECH?

Back 32

Decrease H+ ion secretion by the tubules

Increase excretion of Na+ & H2O

LIMITED DIURETIC Fx

Front 33

what are Carbonic anhydrase inhibitors really used for?

Back 33

to Tx Glaucoma

DIURETIC FX IS LIMITED

Front 34

drugs w/ anticholinergic Fx do what to the bladder?

Tx what?

Back 34

decrease bladder contraction

Tx overactive bladder

Front 35

Finctions of the Renal Sys? (6) - 2 weird

Back 35

1) rid body of impurities/waste, excreting H2O & E-'s

2) reg acid-base balance

3) maintain BP

4) manage circ fluid vol

5) ASSIST IN PRODUCTION OF RBC's

6) CONTRIBUTE TO CA+ METABOLISM

Front 36

avg GFR?

Back 36

125 mL/min

(99+% of filtered plasma = reabsorbed in the tubules)

Front 37

glomerular filtration?

Back 37

the process of E-'s and H2O passing from the vessel through capsular membrane into Bowman's Capsule