Week 8 Flashcards by Alex Ramirez

What enzyme is involved in the synthesis of cholestrol?

GMG-CoA

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Initial response of statin drugs is ____ week and full response normally takes ____

1 week

1 month

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Very low levels of cholestrol can be associated with increased risk of ______ and increased overall ______

cancer

mortality

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A correlation between the use of statin drugs and reduced risk of ____. also there is some evidence that statin drugs may lower the risk of ______ cancer in women and ______ cancer in men

Alzheimers
breast
prostate

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Stain drugs are _____ thus must not be taken while pregant

teratogenic

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_______ the original statin drug which came on the market in 1985. also in generic

Lovastatin

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what is another statin drug

Pravastatin

avaible in generic

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_______ is the most commonly prescribed generic statin drug.

Simvastin

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______ typically produces greater reduction in LDL than previous statin drugs and its #1 selling drug in the US in 2008 with 5.9 billion in sales and 58 million prescriptions written in 2008. Went off patent in 11-30-11

atorvastatin

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_______ is probably the most potent reducer of LDL cholestrol, but also has the highest incidence of myopathy

Rosuvastatin

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_____ is claimed to increase HDL more than other statin drugs and is being marketed particully for type II diabetics as having fewer adverse effects

Pitavastatin

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_______ is a dietary supplement made from Manascus purpureus (______ _____) fermentation of rice. It is a natural yeast that makes a naturally occuring _____-_ reductase inhibitor molecule very similar to Mevacor.

Cholestin
red yeast
HMGCo-A

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A chinease study showed that taking _______ lowers LDL by 25% when taking 13.5 mg/day

Cholestin

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Many studies confirme statin drugs reduce _______ in patients with high cholestrol, but no confirmed cardiovascular disease as well as preventing a second heart attack in those who have had a first MI

mortality

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_______ a new drug that inhibits absorption of cholesterol through intestinal wall. thus it works to lower dietary input of cholesterol into the body. It can be combined with _____ drugs to produce greater reductions in blood cholesterol.

Zetia

statin

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______ high doses of this drug are required and they work by lowering triglycerides thus raising HDL, and lowers LDL.

Niacin

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Adverse effects of Niacin are _____ flushing and i_______ and ____ upset. They can also casue ______ damage. Niacin is aviable as a time release form, which reduces flushing and itiching and this form of drug is known as ______

cutaneous
itiching
GI
Liver
Niaspan

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_______ activates LIPOPROTEIN LIPASE which lowers high blood triglycerides as well as LDL. It increases HDL up to 25% by an unkown mechanism

Tricor

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Adverse effects of Tricor are increased risk of ______ formation, _______ (heart burn 20%), abdominal pain (10%), and diarrhea (7%). Tricor should not be combined with the ____ family because increased risk of myopathy.

gallstone
dyspepsia
statin

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_____ was a drug which caused elevation of HDL. However during phase 3 trials showed that although it raised HDl, it actually increased mortality rate. This is a case of a positive _______ outcome (increased HDL) but a negative ________ outcome (increased mortality)

Torcetrapib
surrogate
clinical

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what is another HDL elevating drug and what phase is it in

Anacetripib

phase 2

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________ is a naturally occuring glycoprotein made in the _____ _____ which stimulates production of red blood cells. It is used primarily in chronic _____ disease patients with anemia to stimualte increased levels of red blood cells. It has also been used to ________ red blood cell growth in anemic cancer patients undergoing chemo. It is a protein and must be given IV or injection

Erythropoietin
adrenal cortex
kidney
promote

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__________ is a synthetic form of a naturally occurring Levothyroxine (T4) hormone made in the ______ gland. Low natural levels of thyroxine can lead to f_____, col intolerance, d_____, Muscle cramps, weight gain, and b______

Levothyroxine
thyroid
fatigue
depression
bradycardia

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Levothyroxine should be taken a half hour before food and once a day. Soy should may hinder the efficacy of this drug. Levothyroxine is one of the few drugs that is given an _____ rating on the teratogenicity scale

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NSAIDS work by inhibiting ______ ______ the enzyme responsible for synthesizing _____ from fatty acids, primarily arachidonic acid.

Prostaglandin | prostaglandins

prostaglandins cause cause

increased sensitivity of pain receptors increased body temp uterine contractions increased platelet aggregation

primary use of NSAIDs is to reduce risk of ischemic strokes and Mis, decrease inflammation, pain, fever, and primary menstrual cramps

___

adverse effects of NSAIDs are stomach ulceration, renal failure, may induce ____ attack, and may reduce efficacy of ____ inhibitor drugs

astma | ACE

what are the two forms of cyclooxyrgenase enzyme

``` Cyclooxygenase 1 (COX-1) Cyclooxygenase 2 (COX-2) ```

COX-1- stimulates- | COX-2 Stimulates-

production of mucous lining of the stomach | inflammatory response

______ is the oldest NSAID still on the market and has been available since 1899. Its primary adverse effect is ___ _____. It is used for analgesia, reduction of fever, reduction of inflammation but not effective in ___ ____.. Because it is an effective inhibitor of the synthesis of ____ _ it has been promoted for reducing the risk of MI's due to its ability ti inhibit platelet aggregation

aspirin stomach ulcers menstural cramps thromboxane A2

Aspirin is common available in two from _____ form and _____ ____. The ____ form is combined with a base such as MgO to speed up the dissolving of the aspirin. People appear to have less stomach pain with this form. The ____ ____ doesn't dissolve in the stomach and does not dissolve until it reachers the alkaline conditions of small intestine. But inhibitor of prostaglandin still inhibits formation of stomach mucous lining and absorption is often ____

``` Buffered enteric coated buffered enteric coated erratic ```

Aspirin side effects include risk of ___ syndrome anaphylaxis, asthma attacks

reyes syndrome-in children with influenza or chicken pox-Reyes syndrome presents with nausea, vomiting, fever and could go to coma or death`

____ (q 4hrs)is more effective in treatment of primary ______ than aspirin. it causes less gastric bleeding than aspirin. There is risk of kidney problems at high dosage in predisposed patients.

Ibuprofen | dysmenorrhea

_______ (q 8hrs) It is available OTC and by prescription at high doses for aches and pains, arthritis and primary ____

Naproxen | dysmenorrhea

____ is a distant fourth place in OTC NSAIDs

Orudis

______ is available in injectable (IM) and oral forms. it is reputed to be the most ____ NSAID, but there is high incidence of stomach ____. It is used primarily after surgery and recommended for short-term therapy (less than 5 days). Half-life of 6 hours

Ketorolac efficacious ulceration

______ is used primarily for short term treatment of acute gout attack. It has a variety of adverse effects besides the usual problem with ulcers, so its not commonly used for other purposes

Indomethacin

What are two COX-2 inhibitors that are no longer on the market and what is one that is still on the market

Bextra Vioxx Celebrex

COX-2 inhibitors do not inhibit platelet aggregation like aspirin odes and hence do not provide protection against MI's. In recent studies showed that the overall mortality rate of patients on COX-2 inhibitors was higher than those on other NSAIDs due to increase in ____ and __ ____. Thats why Bextra and Vioxx were pulled off the shelf. COX-2 and aspirins have been found to be correlated with reduced risk of ____ cancer

strokes and heart attacks | colon

____ is a sulfa drug with some properties similar to the sulfa antibiotics. It can cause a ____ and _____ sensitivity in people sensitive to sulfa drugs although this is not common

celebrex | rash and sun

____ is not an NSAID strictly speaking. It is an analgesic and antipyretic but not an anti-inflammatory. It main advantage over NSAIDS is that it doesn't cause ___ ____. Its action appears to be only in the CNS.

acetaminophen | stomach ulceration

High doses of acetaminophen can cause ____ ____. typical tablet is 325mg which is converted into toxic free radicals products that are detoxified by _______ a natural molecule found in the liver. Higher doses use up______ thus causing liver damage. Treatment is with _______ a modified amino acid. High doses's for long periods of time can cause renal damage or failure.

hepatic necrosis glutathione glutathione acetylcystenine

Acetaminophen is considered safe in pregnant women but a new study shows that it can cause _____ in the children. Tylenol 1,2,3,4 contains APAP+codeine at different doses and require a prescription.

ADHD

DMARD=

Disease modifying anti-rheumatic drugs

DMARD drugs are use to slow down the advance of ______ _____ by inhibiting immune response because NSAIDS don't do use. However DMARD drugs have numerous toxic side effects thus have restricted their use. Some Dr's advocate their use in earlier treatment to slow progression.

rheumatoid arthritis

______ is a DMARD and acts as an antagonist of folic acid which is essential for DNA and RNA synthesis. It is used in treatment of other types of autoimmune diseases (_____) and some types of cancer. It frequently causes nausea, vomiting and diarrhea. It is possibly _____ and can cause kidney failure, and _______ fibrosis.

methotrexate lupus carcinogenic pulmonary

_____ eg. ______ may be used during an acute inflammatory attack but side effects discourage long term use. adverse effects include edema (especially _____), delayed wound healing and O_______

steroids eg. prednisone facial osteoporosis

_______ and ______ are DMARD and both are antibodies that bind to and inhibit ____ ____ _____ (TNF) which is involved in the inflammatory and immune response. They may decrease the ability to respond to ____ and are very e_____. GIVEN twice weekly by SQ. Treats a variety of autoimmune diseases.

Enbrel and humira tumor necrosis factor infections expensive

_____ is an eye drop medication that is a prostaglandin analog that dilates vessels allowing aqueous humor out of the eye thus decreasing internal pressure. Most common drug in treatment of ______

latanoprost | glaucoma

_____ family of drugs have structures similar to serotonin and may act as serotonin agnostic which bind on serotonin receptors in cranial blood vessels and inhibit release of inflammatory molecules. work best if taken upon noticing first symptoms of. Work better if given ____ rather than oral pill

Triptan | SQ

What are three triptan drugs

Sumatriptan Zolmitriptan Rizatriptan

Opioids bind to opioid receptors in the brain U, sigma, and K receptors. The _ receptor is the most important pharmacologically. These receptors can be activated by naturally occurring peptides e____, D______, e______

endorphins dynorphin enkephalin

what are the three must useful effects of opioids

1. Analgesia 2. anti-tussive (cough suppressant) 3. decrease GI motility (Treatment of diarrhea)

______ and ____ (sustained release) is used for serious pain; post-surgical, terminal cancer, post MI. Oral doses are _-_ times IV dosages due to extensive metabolism. regular oral morphine is given q 4h._____ the sustained release has a ____hr half-life

morphine and ms-contin 5-10 Ms-contin 12

PCA stands for

patient controlled analgesia

_____ is a semi-synthetic opioids and is more lipophilic than morphine and hence enters the brain faster than morphine. Not scheduled 1 in most of Europe. With draw can induce nausea, intestinal cramping and it can be treating with methadone or clonidine to ease withdraw.

Heroin

______ has a higher potency than morphine, may have lesser side effects than morphine for some patients. Given PO, SC, IM or IV

Hydromorphone

_______ is metabolized into morphine, which apparently is responsible for most of its analgesic properties. It is a good ______. It is also a semi-synthetic opioid.

Codeine | Antitussive

Since codeine is a prodrug it has to be converted by ____ ___ enzyme and about 7% of the population lacks this, thus codeine is not a good treatment. This enzyme is also inhibited by the SSRI's ___and _____

CYP 2D6 | Prozac and Paxil

If codeine doesn't work since there is a plateau in efficacy at 60mg/dose move up to oxycodone, hydrocodone, and or morphone

______

______ is also combined with APAP or with HOMATROPINE as antitussive. This combo was the most commonly prescribed drug in 2005, second most const commonly written prescription in the US in 2008 with 101 million prescriptions. This drug is also converted to morphine. It is also a semi-synthetic opioid.

Hydrocodone

_____ can also be combined with APAP and has a lower frequency of nausea and vomiting than morphone, but constipation may still be a problem. May be as good as morphine._____ is a long acting BID form. By chewing up this pill resulted in immediate gratification but reformulation stopped this. It is also a semi-synthetic opioid.

Oxycodone | Oxycontin

____ is a synthetic opioid and good for post-surgical pain control, but long term use builds up toxic liver metabolite causing ____. Short half life, less constipation than morphine.

Demerol | convulsions

______ is a synthetic opioid and is available in 3-day transdermal patch (______), buccal lozenges (_______) and IV solution. Very short acting when given IV (1-2hrs).Preferred for ______

Fentanyl Duragesic Actiq Oralet child birth

_______ and or ______ (combo of APAP) very popular for dental pain, but efficacy questioned. Pulled of market due to increased risk of ____ ____

Darvon Darvocet heart arrhythmias

______ and or ____+ APAP pasta as a morphine agonist but also has a non-opioid pain relieving efficacy due to inhibitor of other pain receptors. It has less respiratory depression than opioids

tramodol and tramodol

______ is a moderate cough suppressant without analgesic effect. Low abuse and OTC. It can produce hallucinations in large doses "____-partying"

Robitussin | Robo