Term
| Advantages of using levothyroxine (T4) over Liothyronine (T3) |
|
Definition
| T4 is converted to T3 in tissues (so gives both products); long T1/2 (better compliance/ daily dosing & minimal s/e missing a dose); lab tests readily available |
|
|
Term
| advanced age (>65); cardiac disease; long standing hypothyroidism |
|
Definition
| Risk factors that limit rapid T4 replacement |
|
|
Term
| Levothyroxine (T4) dosing |
|
Definition
| Initial dose 50mcg/day (12.5-25mcg/day for high risk); repeat labs in 5 weeks; adjust dose by 12.5-50mcg; increased dose needed in pregnancy; infants 1-6 mo need very high dose (10-15mcg/kg/day) |
|
|
Term
|
Definition
| Drug of choice for thyroid hormone replacement & suppression therapy- a synthetic thyroid preparation |
|
|
Term
| Levothyroxine (T4) kinetics |
|
Definition
| Vd=10L; extrathyroid pool= 800mcg; T1/2=7 days; oral absorption=80%; bound=99.96%; absorbed best in duodenum & ileum; absorption modified by these intraluminal factors: food, drugs, gastric adicity, intestinal flora |
|
|
Term
| Levothyroxine (T4) preparation attributes |
|
Definition
| stability; content uniformity; low cost; lack of allergic foreign protein; easy lab measurement of serum levels; long half life (7 days- permitting daily dosing); T4 converted to T3 intracellularly (get both in one drug); generic as effective as brand names |
|
|
Term
| Time to reach steady state levels in Levothyroxine (T4) administration |
|
Definition
| Takes 6-8 weeks after start a given dose so make dosage changes slowly |
|
|
Term
| Levothyroxine (T4) monitoring |
|
Definition
| nml growth & development (children); serum TSH; free thyroxine @ regular intervals |
|
|
Term
| Absorption considerations with Levothyroxine (T4) |
|
Definition
| Impaired absorption with certain foods (bran, soy, coffee) and drugs. Administer on an empty stomach (30" before or 1 hr after meals or @ hs) |
|
|
Term
| Levothyroxine (T4) toxicity |
|
Definition
| Directly related to hormone level. In children: restlessness, insomnia, accelerated bone maturation & growth; in adults: increased nervousness, heat intolerance, episodes of palpitation & tachycardia, unexplained weight loss; in chronic overtreatment: increased risk of Afib & accelerated osteoporosis |
|
|
Term
|
Definition
Antihyperlipidemic
HMG-COA Reductase Inhibitor |
|
|
Term
|
Definition
| Atorvastatin, simvastatin, rosuvastatin & pitavastatin (lovastatin, fluvastatin & pravastatin are similiar but somewhat less efficacious) |
|
|
Term
|
Definition
| Inhibit HMG-CoA reductase |
|
|
Term
|
Definition
| Most effective in reducing low-density lipoprotein (LDL). Reduce cholesterole synthesis and up-regulate (LDL) receptors on hepatocyte. Modest reduction in triglycerides |
|
|
Term
| Statin clinical applications |
|
Definition
| Atherosclerotic vascular disease (primary and secondary prevention) and ACS - acute coronary syndromes. |
|
|
Term
| Statin Pharmacokinetics, toxicities and interations |
|
Definition
- Oral - duration 12-24 hours
- High first-pass extraction by the live
- Plasma 1/2 life 1-3 hours (atorvastin,R pitatavastin & rosuvastatin (12-19 hours)
- Toxicity - myopathy, hepatic dysfunction
- Interactions - CYP-dependant metabolizm (3A4, 2C9) interacts with CYP inhibitors |
|
|
Term
|
Definition
- Give at night, because cholesterole synthesis occurs predominantly at night (with the exception of atorvastatin & rosuvastatin).
- Generally absorption is enhanced by food. |
|
|
Term
|
Definition
| Women with hperlipidemia who are pregnant, lactating, or likely to become pregnant should not be given these agents. |
|
|
Term
|
Definition
| Blocks transport protein NPC1L1 and inhibits intestinal absorption of cholesterol and phytosterols |
|
|
Term
| Ezetimibe Clinical Effect |
|
Definition
| Primary clinical effect is the reduction of LDL levels |
|
|
Term
| Ezetimibe Pharmacokinetics and Toxicity |
|
Definition
| Most of drug is excreted in feces, plasma concentrations are substanially increased with administration of fibrates and decreased with cholestyramine or resins. No significant toxicities or drug other drug interactions |
|
|
Term
|
Definition
| Gemfibrozil and Fenofibrate |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Decreases VLDL and TG; increases HDLs; increases lipoprotein lipase activity |
|
|
Term
| Clinical uses of Fibrates |
|
Definition
| hypertriglyceridemia, low HDL levels |
|
|
Term
|
Definition
| GI upset, rash, myopathy, increased incidence of gall stones |
|
|
Term
|
Definition
| Fibrate given 600mg BID and available in generic; absorbs better if taken with food. Half life 1.5 hrs |
|
|
Term
|
Definition
| Brand name Tricor, can be taken once daily, has multiple doses. Is the fibrate of choice for use in combination with a statin. Half life 20 hrs |
|
|
Term
|
Definition
| Interferes with binding of coumadin - reduce coumadin dose by 30%. Avoid use in patients with renal or hepatic dysfunction. Use with caution in patients with biliary tract disease or those at high risk (women, obese, and Native Americans) |
|
|
Term
|
Definition
| a thyroid synthesis inhibitor that is used in the treatment of hyperthyroidism |
|
|
Term
|
Definition
| Methimazole inhibits the enzyme thyroperoxidase, which normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I-) to iodine (I0), facilitating iodine's addition to tyrosine residues on the hormone precursor thyroglobulin, a necessary step in the synthesis of triiodothyronine (T3) and thyroxine (T4). |
|
|
Term
| Methimazole Precautions / Contraindications |
|
Definition
| Use may cause agranulocytosis, hypoprothrombinemia and bleeding, hepatotoxicity |
|
|
Term
|
Definition
| Agranulocytosis, hepatotoxicity, rash, aplastic anemia |
|
|
Term
| Methimazole Monitoring Recommendations |
|
Definition
| CBC, TSH, hepatic function, prothrombin time |
|
|
Term
|
Definition
| Synthetic Thyroid Hormone (T3) used for hypothyroidism |
|
|
Term
|
Definition
| Activation of nuclear receptors resulting in gene expression with RNA formation and protein synthesis |
|
|
Term
|
Definition
Thyorotoxicosis Signs and Symptoms (table 38-4, p. 687)
Grave's Disease
Cardiotoxicity, especially in those with cardiac disease |
|
|
Term
| Liothyronine Pharmacokinetics |
|
Definition
| Very short T1/2 (24hrs), requiring multiple daily doses at higher costs and 3-4x more potent than levothyroxine, more difficult to monitor levels than Levothyroxine, best used for short-term suppression of TSH. |
|
|
Term
| TSH(thyroid stimulating hormone) Regulates |
|
Definition
|
|
Term
|
Definition
| Pituitary and hypothalamus |
|
|
Term
| When TSH is high, what is not responding and what is the TX? |
|
Definition
| When TSH is high the thyroid is not responding, need to increase dose of T4 |
|
|
Term
| When TSH is low, what is being turned off? |
|
Definition
| When TSH is low the anterior pituitary is being turned off by T4 levels |
|
|
Term
| What are use/indications of TSH |
|
Definition
| To screen for thyroid disorders inpt’s with signs/symptoms(palpitations, goiter, unexplained wt loss or gain, obtundation), assess thyroid fxn and to dx hypo/hyperthyroidism, monitor replacement therapy |
|
|
Term
|
Definition
| Colestipol is a large polymeric resin that binds with bile acids in the intestine, forming a complex that is then excreted in the feces. Excretion of bile acids is increased up to 10 times the normal amount with resin administration. When a decreased amount of bile acid is sensed, synthesis of new bile acid is begun via metabolism of cholesterol; this results in decreased availability of cholesterol for the production of plasma lipids. |
|
|
Term
| True or False: Colestipol is useful as the sole treatment for persons with hypertriglyceridemia. |
|
Definition
| False; Colestipol is useful only for isolated increases in LDL. In patients with hypertriglyceridemia, resin treatment may increase VLDL levels. A second agent may need to be added in this case. |
|
|
Term
|
Definition
| Raises HDL, lowers LDL, lowers trigs |
|
|
Term
|
Definition
| Inhibits VLDL secretion, which decreases LDL production |
|
|
Term
| Precautions/ADE's related to Colestipol administration |
|
Definition
| May reduce absorption of fat-soluble vitamins (A, D, E, K); vitamin K deficiency may cause increased bleeding (due to hypoprothrombinemia). May worsen pre-existing constipation. |
|
|
Term
| Colestipol Drug/Drug Interactions |
|
Definition
| Interferes with absorption of several drugs including digoxin, thiazides, warfarin, tetracycline, thyroxine, iron salts, pravastatin, fluvastatin, ezetimibe, folic acid aspirin and ascorbic acid. Other drugs should be taken 1 hour before or at least 2 (preferably 4) hours after the resin. |
|
|
Term
|
Definition
| Cutaneous vasodilation which causes flushing, itching, dry skin, rashes, acanththosis nigricans |
|
|
Term
|
Definition
| Thyroid Hormone antagonist, directly interferes with thyroid hormone synthesis in the thyroid gland by inhibiting iodide incorporation into thyroglobulin; when thyroglobulin is depleted, the circulating thyroid hormone level drops |
|
|
Term
|
Definition
| hepatotocitiy, agranulocytosis, aplastic anemia |
|
|
Term
| Methimazole (Clinical Uses) |
|
Definition
| Antihyperthyroid (to treat hyperthyroidism) |
|
|
Term
|
Definition
Selectively inhibits intestinal absorption of both cholesterol and phytosterols-- reducing LDL levels
(specifically blocks NPC1L1 transport protein. NPC1L1 is essential for intestinal absorption of cholesterol)
*Unique in that it inhibits dietary cholesterol AND the reabsorption of cholesterol excreted in bile (so it inhibits the cholesterol that is already in your body) |
|
|
Term
Ezetimibe/Zetia
(Clinical Uses) |
|
Definition
Used in Hypercholesterolemia: to decrease cholesterol, specifically LDL cholesterol
*often used w/ statin as this will enhance the effect
-Concentration increases substantially when given w/ fibrates
-Concentration decreases when given with resins |
|
|
Term
|
Definition
Minimal ADRs:
-headache
-viral infection
muscle aches
-low incidence of reversible impaired liver/hepatic function
-rare reports of myositis (inflammation of muscle tissue)
**OF all the cholesterol meds, this one is safest for the LIVER |
|
|
Term
| Thyroid Stimulating Hormone (TSH) |
|
Definition
Thyrotropic hormone that stimulates T4 & T3 synthesis and release from the thryoid.
Regulated by the pituitary and hypothyalamus * |
|
|
Term
|
Definition
Normal: 0.4-4
When high: thyroid is not responding (hypothyroidism) and needs to increase dose of T4
When low: anterior pitutary is "turned off" by T4 levels (hyperthyrodism) |
|
|
Term
| Types of HMG-CoA reductase inhibitors (statins) |
|
Definition
| Lovastatin, Simvastatin, Pravastatin, Fluvastatin, Atorvastatin, Cervastatin |
|
|
Term
| Statins (HMG-CoA reducatase inhibitors) MOA |
|
Definition
| Competitive inhibition of liver enzyme HMG CoA reductase, induces an increase in high affinity LDL receptors. This increases the catabolic rate of LDL and the liver extraction of LDL precursors (VLDL). End result: Reduction in plasma LDL |
|
|
Term
|
Definition
| Liver dysfunction is most common- increased liver enzymes, increased CK from skeletal muscle: may lead to muscle pain, rhabdomyolysis. Pregnancy category X |
|
|
Term
|
Definition
| Liver enzyme levels prior to starting and regularly during therapy, CK levels, also lipid monitoring to ensure therapy goals are being met |
|
|
Term
|
Definition
| Indicated as lipid lowering agents (HDL, LDL, VLDL, and triglycerides) |
|
|
Term
|
Definition
Inhibits very low density lipoprotein (VLDL) which reduces the production of low density lipoprotein (LDL) and also reduces triglyceride levels.
The reduction in VLDL occurs, possibly, by reducing the flux of free fatty acids to the liver. |
|
|
Term
|
Definition
| Used in combination with other resin or reductase inhibitors it can be used in treatment of genetic high cholestorl as well as other forms of hypercholesterima, hyperlipidemia and sysbetalipoproteinemia. |
|
|
Term
|
Definition
Most common: Flushing after each dose during inital days of administration, itchy skin, rashes, dry skin or mucous membranes, nausea and abdominal pain.
Rare/Severe: hepatotoxicity, increase in levels of aminotransferase (therefore baseline hepatic pannel should be done), increase in insulin resistance, hyperuricemia and arrhythmias |
|
|
Term
|
Definition
|
|
Term
| Liothyronine (Clinical Use) |
|
Definition
| Best use for short term suppression of TSH. Short half life. Requires mult. daily doses. Increased cost. Difficult to monitor. |
|
|
Term
|
Definition
| Tremor, sweating, chest pain, tachycardia. Not for use with patients with heart disease. |
|
|
Term
|
Definition
Omega-3 fatty acids found in fish oils, (not plant sources) activate peroxisome
proliferator-activated receptor-alpha (PPAR-α) and can induce profound
reduction of triglycerides in some patients. Omega-3 fatty acids are available
over the counter or as a prescription medication (Lovaza) containing ethyl
esters of omega-3 fatty acids. |
|
|
Term
| Omega-3 fatty acids (Clinical Use) |
|
Definition
Omega-3-acids are used together with a proper
diet to lower triglycerides. They also have anti-inflammatory and antiarrhythmic activities. |
|
|
Term
| Omega-3 fatty acids (ADR) |
|
Definition
Bleeding, SOB, difficulty swallowing, dizziness,
tachycardia, skin rash, weakness, chest tightness |
|
|
Term
|
Definition
| Binds bile acids in the gut by preventing reabsorption thereby increasing cholesteral breakdown. Also upregulates LDL receptors |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| ↓VLDL, ↓ LDL; PPAR-α Ligand up-regulate LPL, apo A-I, apo A-II; down-regulate apo C-III; ADRs = rash, GI upset, myopathy, arrhythmia, hypoK+, ↑aminotransferase, ↑ alkaline phospatase, ↓WBC, ↓hematocrit. Avoid with renal/hepatic dysfunction. |
|
|
Term
|
Definition
| Binds to bile acids in the gut and prevents reabsorption of cholesterol by increasing choleterol catabolism. This leads to increased uptake of LDL and IDL by the LDL receptors |
|
|
Term
|
Definition
| primarily used in patients with primary hypercholesterolemia, leading to a 20% decrease in LDL in patients with maximum dosage. They are also used to treat digitialis toxicity and pruritius |
|
|
Term
| Colestipol Pharmakinetics |
|
Definition
| Available as in a granular preparation, and a gradual increase from 4 or 5g/d to 20g/d is recommended. Total doses of 30-32g/d may be needed for maximum effect. Granular Colestipol is mixed with juice or water and then allowed to hydrate for one minute. It is also availabe in 1g tablets that must be swallowed whole, with a maximum dose of 16g per day. |
|
|
Term
| Colestipol Adverse Reactions |
|
Definition
| Constipation and bloating complaints are common, with heartburn and diarrhea also reported. Can interfere with other medications and vitamins. |
|
|
Term
| Statins Mechanism Of Action |
|
Definition
| Competitive inhibitors of HMG CoA reductase, the rate limiting step in cholesterol biosynthesis. They occupy a portion of the binding site of HMG CoA therefore blocking access of this substrate to the action site on the enzyme. |
|
|
Term
|
Definition
| Atherosclerotic vascular disease--both primary and secondary prevention; acute coronary syndromes |
|
|
Term
|
Definition
| Oral route; duration is 12-24 hours; Majority of cholesterol synthesis occurs at night |
|
|
Term
| Statins Adverse Reactions |
|
Definition
| Myopathy; hepatic dysfunction; statin-induced myalgisa, proteinuria; can effect glucose metabolism |
|
|
Term
|
Definition
| Reduces cholesterol synthesis; decreases LDL receptor turnover; decreased VLVD; modest HDL increase, modest reduction in triglycerides |
|
|
Term
|
Definition
A form of polyunsaturated fats the body derives from food and in some cases supplements. Is liquid soluable at room temperature, the body converts these fatty acids consisting of Alpha Linolenic Acid (ALA), Eicosapentaenoic Acid (EPA), and Docosahexaenoic acid (DHA) also known as n3 Polyunsaturated fattyacids and are incorporated into cell membranes and dictates how cells grow, respond and maintain a high degree of fluidity. They inhibit Cox 2 enzymes producing anti-inflammatory responses, aid in prostaglandin production to lower B/P, blood clotting and nerve
transmission, and activate the sphingomyelinase enzyme that causes cancer cell death. Other effects includes: lowering cholesterol and triglycerides levels, |
|
|
Term
|
Definition
| Also known as Fish Oil, Fish Oil Supplements, Cod Live Oil, Marine Oil |
|
|
Term
| Foods High in Omega 3 Fatty Acids |
|
Definition
dark green leafy vegetables,certain vegetable oils, flaxseed, walnuts, cold-water fish, tofu, grass-fed
beef, and soybeans. |
|
|
Term
| Omega 3 - Adverse Effects |
|
Definition
| Hypersentistivity, increased risk of bleeding, hemorrhagic strokes |
|
|
Term
|
Definition
| blocks sterol transporter NPC1L1 in intestine, inhibiting cholesterol reabsorption |
|
|
Term
|
Definition
| Low incidence; hepatic dysfunction and myositis can occur |
|
|
Term
| Ezetimibe Pharmacokinetics |
|
Definition
Reaches peak blood levels in 12-14 hours.
Half-life is 22 hours.
Undergoes enterohepatic circulation.
Approximately 80% of the drug is excreted in feces. |
|
|
Term
|
Definition
| Elevated LDL: average reduction in LDL with ezetimibe alone in patients with primary hypercholesterolemia is ~18%. Phytosterolemia. |
|
|
Term
|
Definition
| Peroxisome proliferatior-activated receptor-alpha (PPAR-alpha) agonists, Which means is decrease secretion of very low density lipoproteins (VLDL) and increase lipoprotein lipase activity and increase HDL's Examples: Fenofibrate, gemfibrozil |
|
|
Term
|
Definition
| hypertriglyceridemia, low HDL |
|
|
Term
| Fibrates pharmacokinetics |
|
Definition
| Oral route, duration 3-24 hours, should be avoided in patients with hepatic or renal dysfunction |
|
|
Term
|
Definition
| myopathy, hepatic dysfunction, arrythmias, hypokalemia, nausea, skin rash, gall stones |
|
|
Term
|
Definition
| Stimulates an adenylyl cyclase-mediated mechanism in the thyroid cell to increase the synthesis and release of T3 and T4 |
|
|
Term
|
Definition
| Regulated by the pituitary and hypothalamus |
|
|
Term
| Drugs that inhibit TSH secretion without induction of hypo- or hyperthyrodism |
|
Definition
| Dopamine, bromocriptine, levodopa, corticosteroids, somatostatin, metformin |
|
|
Term
| Drugs that inhibit thyroid hormone synthesis or release with induction of hypo- or hyperthyroidism |
|
Definition
| Iodides (including amiodarone), lithium, aminoglutethimide, thioamides, ethionamide, tyrosine kinase inhibitors (sunitinib, sorafenib, imatinib), HIV protease inhibitors |
|
|
Term
|
Definition
| Decreases VLDL and LDL levels, Liproprotein(a) Lp(a). Significantly raises HDL levels. |
|
|
Term
|
Definition
| Inhibits Very Low Density Lipoprotein (VLDL) secretion which decreases production of LDL. Increased clearance of VLDL via the Lipoprotein Lipase (LPL) pathway results in decreased triglycerides. Excretion of neutral sterols in the stool results as cholesterol moves from tissue pools to a new steady state. Plasminogen goes up causing fibrinogen to go down. Niacin inhibits intracellular lipase of adipose tissue via receptor mediated signaling. This may reduce VLDL by decreasing the flux of free fatty acids to the liver. |
|
|
Term
|
Definition
| Cutaneous vasodilation (feeling flushed) nausea, pruritus, rashes, dry skin or mucous membranes. Acanthosis nigricans (darkening of skin in body folds and creases) contraindicates niacin d/t its association with insulin resistance. GI upset, avoid in patients with severe peptic disease. |
|
|
Term
|
Definition
| It is a T3 thyroid hormone. It activates nuclear receptors leading to increased RNA formation (similar to Levothyroxine). Increased RNA synthesis leads to increased protein synthesis and formation. |
|
|
Term
| Liothyronine clinical use |
|
Definition
| Treatment of Hypothyroidism |
|
|
Term
| Liothyronine Pharmacokinetics |
|
Definition
| Faster onset and shorter half life than Levothyroxine. It is absorbed best in the duodenum and ilium. Absorption is effected by food, so it is recommended to take it without food in the stomach. |
|
|
Term
| Liothyronine adverse effects |
|
Definition
| Similar to hyperthyroidism or Graves' disease. Flushed skin, thin hair, retraction of upper eye lid, increased heart rate, nervousness, weakness... etc. |
|
|
Term
|
Definition
Inhibits the enzyme thyroid peroxidase (which normally acts in the thryroid hormone synthesis by oxidizing iodide to iodine) by facilitating iodine's addition on the hormone precursor thyroglobulin, a necessary step in the synthesis of T3 and T4.
Inhibits peripheral deiodination of T4 and T3. |
|
|
Term
|
Definition
|
|
Term
| Methimazole Adverse Effects |
|
Definition
| Nausea and vomiting, GI distress, rash, agranulocytosis, hepatitis (PTU blck box), hypothyroidism, loss of hair, loss of taste, joint and muscle pain, decreased WBC, decreased platelets, sore throat and/or high fever |
|
|
Term
|
Definition
| synthetic form of thyroxine, T4 is converted to T3 intracellularly. T4 &T3 then bind to thyroid receptor proteins in the nucleus which leads to increased formation of RNA and protein synthesis |
|
|
Term
| Levothyroxine Clinical Use |
|
Definition
| Thyroid replacement for patients with hypothyroidism |
|
|
Term
| Levothyroxine Pharmacokinetics |
|
Definition
| Long half-life of 6-7 days, once daily dose is needed (monitor TSH in 5 weeks), Pregnancy category A (increased dosages are needed) |
|
|
Term
| Levothyroxine risk factors |
|
Definition
| advanced age, cardiac disease, long standing hypothyroidism |
|
|
Term
| STATINS (HMG CoA Reductase Inhibitors) |
|
Definition
| Inhibit liver enzyme HMG CoA reductase, which is required for cholesterol synthesis, thereby increasing the extraction of LDL resulting in reduction of serum LDL. Other effects include decreased vascular inflammation, increased plaque stability, decreased triglycerides, increased HDL. ADR include increased liver enzymes, rhabdomyolosis and elevated creatinine kinase. Statins are pregnancy category X and need to be avoided during pregnancy and breastfeeding. |
|
|
Term
|
Definition
Niacin or Vitamin B3 is used to decrease VLDL and LDL levels,
and to increase HDL levels. It also has anti-atherosclerotic properties. MOA:
Increased clearance of VLDL via LPL (lipoprotein lipase) pathway. It is
excreted in the urine unmodified and as several metabolites. |
|
|
Term
| Niacin therapeutic use and dose: |
|
Definition
Combined with a resin or reductase inhibitor, normalizes LDL
cholesterol (heterozygous familial hypercholesterolemia) in a dose: 2-6
g/daily. Other types of hypercholesterolemia and hypertriglyceridemia= 1.5 to
3.5 g/daily. |
|
|
Term
|
Definition
Harmless cutaneous vasodilation after first doses or when
dose increased. Aspirin 81-325 mg or Ibuprofen helps preventing this prostaglandin
mediated effect. |
|
|
Term
|
Definition
| A type of thioamide antithyroid agent that inhibits thyroid peroxidase reactions. It blocks iodine organification, and it inhibits peripheral deiodination of T4 and T3. |
|
|
Term
| Methimazole: Indications for use |
|
Definition
| Used to treat hyperthyroidism (Graves' disease). Drug is most useful in young patients with small glands and mild disease. Administered until the disease goes into spontaneous remission. |
|
|
Term
| Methimazole: Side effects |
|
Definition
| Nausea, GI distress, rash, agranulocytosis, hepatitis, hypothyroid. Methimazole is preferred over proprylthiouracil (PTU) because of lower risk of serious liver injury and can be administered once daily. |
|
|
Term
| Cholestipol (Pravastatin) |
|
Definition
| MOA: reversible competitive inhibitor of HMG-CoA. Blocks synthesis of nonsterol metabolites necessary for normal cell proliferation can survival. Decreases production of melvalonic acid from HMG-CoA resulting in a decrease in hepatic cholesterol synthesis. This leads to a compensatory increase in the expression of high affinity LDL receptors on hepatocyte memebranes and stimulation of LDL catabolism. Cholestipol produces the lowering of plasma total and LDL cholesterol levels. |
|
|
Term
| Cholestipol (Pravastatin) uses: |
|
Definition
| Dyslipidemia and pervention of cardiovascular disease. |
|
|
Term
| Cholestipol (Pravastatin) ADR |
|
Definition
| impaired cognition, dizziness and rash, dermatitis, new onset DM2, glucose reg disorder, gynecomastia, diarrhea, N/V, pancreatitis, cholestatic jaundice syndrome, increased liver enzymes, liver failure, increased Cr Kinase, Rhabdomyolysis, myalgia, muscle cramps, and aches, tendinitis |
|
|
Term
|
Definition
| Tagamet, Cyclosporin, Tricor, Lopid, Cholestyramine, Niacin |
|
|
Term
|
Definition
Thyroid Stimulating Hormone.
Released by the pituitary gland to stimulate the thyroid to synthesize and release T3 and T4 in a negative feedback mechanism. |
|
|
Term
| Fibrates (Fibric Acid Derivatives) |
|
Definition
| Interact with receptor sub-type (PPAR) peroxisome proliferator-activated receptor alpha to systhesize increased lipoprotein lipase (LPL) and reduce production of apolipoproyein C-III. |
|
|
Term
| Fibrates (Fibric Acid Derivatives) |
|
Definition
| accelaerate the clearance of VLDLs and reduce levels of triglycerides (TG) |
|
|
Term
| Fibrates (Fibric Acid Derivatives) |
|
Definition
| Increase HDLs through activation of PPAR alpha which increaes production of A-I and II. |
|
|
Term
| Fibrates (Fibric Acid Derivatives) |
|
Definition
| Gemfibrozil, fenobibrate and fenobibric acid |
|
|
Term
| Fibrates (Fibric Acid Derivatives) |
|
Definition
| ADRs- N,V,D, Gallstones, myopathy, liver injury, rash |
|
|
Term
| Fibrates (Fibric Acid Derivatives) |
|
Definition
| Removes warfarin from plasma albumin, increases coag effects. PT (INR) need to be monitored. Should not use in combo with statins because of the myopathy risks. |
|
|
Term
|
Definition
| A synthetic preparation of T4 (thyroxine). Given to correct hypothyroidism. Converts to T3 in cells. Takes 6-8 weeks for maximum effect to be seen. Should be given on an empty stomach. ADRs include signs of thyroid excess such as increased nervousness, heat intolerance, palpitations and tachycardia, and unexplained weight loss. |
|
|
Term
|
Definition
| Used to treat hypothyroidism. Synthetic thyroid hormone T3 (triiodothyronine), it is important part of central nervous system development. It stimulates oxygen consumption by most body tissues, accelerates the basal metabolic rate and the metabolism of carbohydrates, proteins and lipids. |
|
|
Term
| Liothyronine Pharmacokinetics |
|
Definition
| Moderately protein bond, excreted by kidneys, when given IV a 95% bioavailability in 4 hours. Also dosed orally. Short half-life. Fast onset. Not considered drug of choice for treatment of hypothyroidism. |
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Term
| Liothyronine Clinical Considerations/ADR |
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Definition
| This drug may cause cardiac dysrhythmia, sweating symptom, headache, or thyrotoxicosis. Monitor for patient for signs/symptoms of hyperthyroidism. Monitor labs of serum T3 and TSH level not as easily monitored. Avoid in patients with cardiac disease. |
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Term
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Definition
| A lipid lowering agent that inhibits sterol absorption. MOA: Prevents intestinal absorption of dietary and biliary cholesterol by inhibiting cholesterol transport across the intestinal wall. Can be used alone or in combo with statins. Very long half life (22hrs) which increases compliance. Pregnancy category C. ADR: Very few, possible muscle aches, headache, or viral infection. Is not metabolized by CPY P-450 and therefore has no liver reactions. Has no drug interactions with vitamins. |
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