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111 Cards in this Set
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Pilocarpine
Category? Use? |
Cholinergic: Direct Acting Muscarinic.
Stimulates saliva |
Slide 3 test: stimulates saliva
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Nicotine
Category? Use? |
Cholinergic: Direct-acting nicotinic
Induces skeletal muscle contraction. Works on BV's, by binding to para-symp receptors. |
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Physostigmine
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Cholinergic: indrect acting
Inhibits cholinesterase, increases AcH levels @ the synapse... |
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Define pharmocology
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Effects of chemicals on live tissue
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What is BASIC pharmocology?
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Effects of useful chemicals on cell cultures / animals (not in humans)
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What is CLINICAL pharm?
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Studying effects in humans
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What is pharmacoKINETICS?
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What the BODY does to the DRUG. (how it gets in, distribution, metabolism, excretion)
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What is pharmacoDYNAMICS?
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What the DRUG is doing to the BODY. Conformation changes / activating G-proteins / dose-response relationships...
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What drug shouldn't be taken with dairy? Why?
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Tetracycline. Kelates (attaches) to di and tri cations (Ca/Mg/Al/Fe)
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What drugs have a high first-pass rate?
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Morphine / Fentanyl (60-90%)
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What effect do drugs with active metabolites have? Name drug with active, and without active.
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Active = lasts longer. Diazepam lasts 85hrs in elderly.
No active = lasts shorter (Oxazepam) |
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What do people take Warfarin for?
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Atrial fibrillation. Has NO anti-arrythmic activity, it's an anticoagulant.
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What do people take Diazepam for?
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Anxiety, and as a sleeping pill.
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What drugs cause gingival hyperplasia?
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Prazosin, Phenyton (Dilantin), Cyclosporine (Sandimmune)
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Also Ca-channel blockers, tx of high BP and angina.
Hifedipine, verapamil, diltiazem |
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How does Prazosin (Minipres) used and work?
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Blocks alpha-1 receptors, decreases blood pressure via vasodilation
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Zolendronic Acid (Zometa): whats is it used for?
What's a major problem associated with it? |
Bisphosphonate for osteporosis, and bone cancers.
Can cause osteonecrosis of the jaw after invasive bone-exposing dental procedures. |
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Contraindication for atropine?
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Glaucoma
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What allergy is a red flag for prescribing percodan?
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Aspirin. Percodan = oxycodone + aspirin
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Contraindications for the antibiotic metronidazole? (Flagyl)
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Drinking alcohol (get acetaldehyde buildup, feel sick), warfarin (inhibits enzyme that metabolizes it)
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Contraindications for Fiorinal? (a barbituate)
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Fiorinal = Aspirin + Butalbital.
Butalbital increases breakdown of warfarin. Subtherapeutic |
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What receptors does Epi stimulate?
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Alpha 1 (vasoconstriction)
Beta 1 (increase HR) Beta2 (skeletal muscle bv's and internal organs bv's |
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What does Atropine do? Who don't you prescribe it to?
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The saliva-drier. Anticholinergic/antimuscarinic.
Patients with glaucoma. |
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Metronidazole (Flagyl): what can't you do when you're on it? Why?
If you are currently on ________ , metronidazole could kill you. |
Drink. Interferes with acetaldehyde dehydrogenase, get acetaldehyde buildup.
Disulfiram/Anabuse = does the same thing. Metronidazole also interferes with WARFARIN metabolizer, +++warfarin --> bleed to death. |
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Warfarin + Fiorinal?
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Fiorinal = Aspirin + Butalbital.
Butalbital increases warfarin enzymes, --> Warfarin becomes SUBTHERAPEUTIC. (get clots) |
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Beta 1 effects?
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Increased HR / force
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Beta 2 effects?
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Bronchodilation.
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Problem with nonselective beta-blocks?
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Asthmatics, could suffocate and die.
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Why can't you give epi to someone on propranolol?
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Propranolol blocks out beta1/2. Epi then works on Alpha1 only,
--> VASOCONSTRICTION everywhere. BP sky rockets. |
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Bromfenact:
why did it get pulled off market in phase 4? |
Liver toxicity with longterm use.
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Cisapride:
why did it get pulled off market? |
Treated GERD, buttttt:
Ventricular fib and torsades de pointes. |
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Terfenadine:
- significance of the drug? - Why it got pulled? |
First non-drowsy antihistamine (doesn't cross BBB)
- Ventricular arrythmias. |
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Phenylpropynolamine
What was it used for? Why did it get pulled? |
Nasal decongestants.
An indirect symapthomimetic. Increased STROKES in young women. |
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Cervastatin:
What is it used for? Why did it get pulled? |
Lowers LDL (bad kind), slightly raised HDL.
Cause muscle aches (myalgia), but some got rhabdomyolysis (muscle breakdown-->renal failure) |
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Rofecoxib
What is it used for? Why did it get pulled? |
NSAID for arthritis
Caused strokes and heart attacks. |
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Examples of DEA Class II Drugs?
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Oxycodone
Stanozol (anabolic steroid) Methylphenadate (Ritalin) |
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What's a DEA Class III Drug?
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Vicodin. (Hydrocodone + acetaminophen)
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Some DEA Class IV Drugs?
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Benzodiazepines
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A DEA Class V Drug?
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Cough preparations with little bit of codeine
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What about drugs not in Classes 2-5?
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Safe and no abuse potential. Not controlled substances.
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Pregnancy Category A: which drugs?
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Vitamins, NaF...very few.
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Pregnancy Category B: which drugs?
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Lidocaine / ibuprofen (in 1st/2nd trimesters)
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Pregnancy category C: which drugs?
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Mepivocaine and Eupivocaine
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Pregnancy category D: which drugs?
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IBUPROFEN in 3rd trimester, bleeding during birth and premature ductus closure
TETRACYCLINE:: slows fetal bone dev Chemotherapy/Anticonvulsants Benzos |
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Pregnancy category X:
What does the category mean? Which drugs? |
Benefits do not outweigh the risks/effects.
ACNETANE --> mental retard in fetuses CYTOTEC --> Ulcer prevention, caused spontaneous abortions THALIDOMIDE: for morning sickness, causes phocomelia (arm deform) BENZOS |
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Which drug is actually sped up when taken with fatty foods?
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Griseofulvin - for feet fungus
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What drugs are absorbed in the stomach?
Are they weak acids or bases? |
Aspirin, Propionic Acid (ibuprofen)
Weak acids, they are uncharged in stomach |
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Name some weak base drugs
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-caines, opioides (morphine / codeine)
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What drugs are charged no matter what the pH?
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Ions and Quaternaries. Must be INJECTED!
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Name drugs that must be injected and why.
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CURARE: charged
PENICILLIN-G: stomach acids destroy it INSULIN: stomach acid. |
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Why is morphine difficult to administer orally?
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It has a very high first pass effect. Most of drug metabolized.
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An antiarrythmic drug you might not suspect?
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pure Lidocaine
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A super-morphine?
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Fentanyl. Available as a lollypop.
Risk: respiratory depression. Safety: high first-pass effect. |
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What makes N2O a safe drug?
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It leaves the body very quickly.
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What's Nitroglycerine used for?
Nitric Oxide? (NO) |
Angina attacks, it is a vasodilator.
NO is also a vasodilator |
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What does biotransformation usually accomplish?
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-more WATER soluble, more POLAR
-decreased halflife |
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Diazepam: an A-S-H drug.
Why does it last long? Is there an alternative? |
Antianxiety, Sedative, Hypnotic
Has active metabolites Oxazepam: w/o the active metabolites. (lasts shorter tho) |
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What does codeine become once it is absorbed?
Why do 10% not respond to it? |
Morphine. Codeine is a prodrug.
They are CYP2D6 deficient, can't convert to morphine. |
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Statins: method of action?
Bad side effect? What food can't you eat? |
HMG-CoA reductase inhibitors
Effect: m.myalgia, rhabdomyolysis Food: NO GRAPEFRUIT JUICE. Inhibits the enzyme to break statins down. |
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CYP Effects: when are they largest?
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When drug administered orally/ingested
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What is a QUANTAL response?
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All or none. 5% of drugs.
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When 50% of the receptors are bound you get....
And how do spare receptor systems affect it? |
get 50% maximum effect. (EC50)
Spares: EC50 becomes less than the Kd. |
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K3 value:
1 = ? 0 = ? |
1 = agonist
0 = antagonist |
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What is the THRESHOLD dose?
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Dose @ which you first see a response.
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Dose-Response Curves:
What does left-shifted mean? |
more potent, takes less drug to reach same maximum.
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Dose-Response Curves:
What is another name for the maximal effect? |
Intrinsic activity (Emax)
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Oxycodone vs. Codeine.
Difference in Emax / potency? |
Same Emax, but Oxycodone is more potent.
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What is Diclofenac?
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an NSAID that Europe loves to use.
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What drug fixes an opioid overdose?
What happens to graph when added to oxycodone? |
Naloxone, an opioid receptor antagonist.
When mixed: shifts curve to right. |
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What is Buprenorphine used for?
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A partial opioid agonist. Has higher affinity that the opioid to receptors, but less of an effect. Good for weening people off.
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Difference between Curare and Succinylcholine?
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Curare = non-depolarizing muscle paralysis.
Succinylcholine = depolarizing. Muscles work themselves out and then freeze. Lasts less, unless atypical cholinesterases (lasts 24hours, can't reverse) |
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What type of antagonism involves RECEPTORS and is completely reversible with enough agonist?
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Competitive
Ex: curare/naloxone |
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What type of antagonism involves RECEPTORS and cannot be reversed with agonist?
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Non-competitive.
Ex: succinylcholine |
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What type of antagonism involves a drug binding to another drug to block it or block its absorption?
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Chemical.
Ex: Tetracyclines and cations (dairy) |
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What type of antagonism is when one drug does the opposite of another drug, and works on a totally different receptor?
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Physiologic.
Ex: alcohol = -CNS. caffeine = +CNS |
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INR for warfarin: what # is normal?
What number is too high for tx? |
Normal = 1
3.5+ is too high to treat. |
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What happens when a patient on warfarin takes ibuprofen?
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Both drugs compete for plasma proteins to bind to, and are highly protein bound.
Warfarin's normal 1% free may jump to 4% free, could bleed to death. |
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What's a problem when you give someone an NSAID who is on Glyburide?
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Glyburide is a hypo-glycemic agent, highly protein bound in blood.
On an NSAID, %free of glyburide can increase to overdose levels, become hypoglycemic (very bad). |
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Talk about Penicillin's halflife and dosing.
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Very short halflife (30mins)
Gets actively excreted, and unchanged by the body! Dose every 6 hours because it does such a good job killing bacteria. An exception to the "dose on the halflife" rule |
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Probenacid (Uricosuric): what does it do and what does it compete with?
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Treatment of gout/arthritis. Increases urinary excretion and its acidity.
Competes with excretion of penicillin, so penicillin acts on body longer. |
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Why is Lithium a dangerous drug in tx of bipolar disorder?
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Low therapeutic index.
CNS and kidney toxicity at high doses. |
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What should you NOT prescribe someone who is taking Lithium?
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NSAIDs. They compete with active secretion of lithium. Lithium levels go up++, --> toxicity/ataxia.
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A drug won't make it into the kidney for excretion is it is....
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Still very LIPID-sol. Will get reabsorbed into the bloodstream and not get excreted.
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Barbituates:
Weak acid or weak base? High or low therapeutic index? What's the antagonist? |
Weak acid.
LOW therapeutic index There is NO antagonist for barbituates. |
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How to reverse a diazepam overdose?
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Flumazanil
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For weak acid drugs, what can you do to enhance their excretion in an overdose?
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Alkalinize the urine (creates more CHARGED form) --> excretion.
Give Sodium Bicarbonate. Called "ion-trapping" |
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Acetazolamide: use?
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High altitude sickness.
Also increases pH of urine. |
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What is First-Order kinetics?
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At every halflife, 50% of drug is removed from the body.
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What is Zero-Order kinetics?
Ex? |
Drug gets removed at a constant rate from the body. The amount present DOESN'T MATTER.
There is more drug than enzyme can keep up with. ALCOHOL. |
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Sweat glands:
Anatomy/receptors? |
Sympathetic anatomy, but muscarinic cholinergic receptors!
Respond to PS drugs. |
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Curare vs Succinyl-Choline
How to reverse block? ** |
Curare: anticholinesterase
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What drugs are nerve gases?
What's the antedote? |
Anticholinesterases. First excite, then paralyze and get all the PS effects (SLUDGE)
Atropine antedote, blocks the PS effects. |
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What's the use for Mecamylamine and Trimethaphan?
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Used in a severe hypertension emergency, blocks Nicotinic-N receptors (PS and S block)
Blocks the system that dominates the organ. Heart/BV's: sympathetic gets blocked. --> Decrease HR and Vasodilate. |
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The ideal BP lowerers working with alphas....
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Would BLOCK alpha 1, and STIMULATE alpha 2.
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Chronotropic / Ionotropic
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Chrono = HR
Iono = force |
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Anticholinesterases: what is their method of action?
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INDIRECT. They interfere with the breakdown of Ach in the synapse --> Ach sticks around longer.
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Muscarinic cholinergic agonists: method of action?
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DIRECT (always?)
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Anticholinesterases, is covalent or noncovalent linkage worse?
Do they do anything to blood vessels? |
Covalent. Nerve gases / insecticides.
BV's: No effect |
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What common characteristic do abused drugs have?
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High lipid-solubility. Means that is gets across the BBB very easily.
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Name the uses of a beta blocker.
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Migraine headaches
Angina Hypertension Cardiac arrythmia |
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How do you dose based on someones weight?
What's a problem with BMI dosing? |
Adult dose x (their weight)/150.
Ex: 200mg x (300/150) = 400mg. Obese = high BMI but less water than someone with a lot of muscle. More likely to overdose. |
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Significance of Pentazocine?
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mixed opioid agonst/antagonist.
Women found it effective, but not men. *check* |
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Methemoglobanemia: what's the problem?
What drugs make it worse? What's the antedote? |
10% met (Fe3+) (compared to 1-2%)
Oxidizing drugs = BAD. Sidanest / Prilocaine / Benzocaine Antedote: Methylene blue. |
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What's a problem with a chronic pain patient taking opioids?
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PharmacoDYNAMIC tolerance. Receptor density increases.
Dose may need to be upped to get same response, but dose may be lethal. |
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Pharmacokinetic tolerance?
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Drug speeds up its metabolism/enzymes.
Alcohol and Barbituates do it. |
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What can't you prescribe to someone on SSRI's?
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Codeine. Depends on 2D6 to get active, but SSRI's interfere and making codeine ineffective.
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What are MAOI's? What can't you do on them? Why?
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Antidepressants
Eat TYRAMINE (list of 50-60 foods). Tyramine is a SYMPATHOMIMETIC drug, and is normally inactivated by MAO in the stomach! No MAO = tyramine gets absorbed and get over-release of NE everywhere. (increase BP and cardiac arrythmias) |
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How does cocaine work? (direct? indirect?)
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Indirect.
Stimulates NT release Blocks NT reuptake Sensitizes the receptors. |
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What is Dantrolene used for?
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Reverse malignant hyperthermia children can often get from certain triggering drugs. It decreases Ca release in muscles.
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What was the problem with Tholidamide?
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Used for morning sickness.
Caused arm/leg deformities |
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Can animals be used to determine dosing in humans?
What about teratogenicity? |
No for both. Many are species-dependent.
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Name the 2 MAOI's discussed in lecture
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Trade names:
Nardil Parnate |
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