Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
49 Cards in this Set
- Front
- Back
|
Drugs that were removed during Phase 4
|
Duract - Analgesic gave liver toxicity
Phenylpropylnolamine - Decongestant in cold/cought medicine gave young women strokes Cerivastatin - Cholesterol drug that lead to rhabdomyolysis Vioxx and Bextra - Cox-2 inhibitors that increased strokes and heart attacks FenPen Seldane - Non-sedating histamine that caused ventricular arrhythmia. Taken off the market because mixing seldane pro-drug (turns into allegra) with 3A4 inhibitor lead to heart problems Toradol - Great for kidney stone pain but given phase 4 warning due to GI bleeds |
|
|
Drugs that impact the fetus
|
A- prenatal vitamins and sodium fluoride
B - "caines" - causes bradycardia and respiratory depression C - advil and motrin - fetal bleeding and ductus closing D - tetracycline - tooth discoloration and inhibit bone growth. Chelate with ions to limit effect X - Cytotec - Abortion |
|
|
Class 1 Drugs
|
Warfarin -Blood thinner inhibits synthesis of Vitamin-K clotting factor. Give if someone has atrial fibrillation
Propranalol - Non-specific Beta blocker. Minipress - Alpha blocker. People can pass out if the get up too quick Nifedipine and Calan - Vasodilate and block Ca++ channel to reduce BP can cause gingival hyperplasia Vallium - Anti-anxiety works through GABA-B and allows Cl- to come in. Side effect is sleepy and loss of control Elavil - Anti-depressent blocks reuptake of NOR and setotonin. Blocks M.C leading to xerostomia. Good for TMJ pain Atropine - M.C. receptor antagonist dries the mouth. Don't give to glaucoma patients |
|
|
Class 1 Continued
|
Zolendronic Acid - For osteoporosis cause necrosis of the jaw
Metronidazie - Good for strict anerobes blocks conversion of acetaldehyde to alcohol. Can inhibits warfarin enzyme so warfarin builds up Barbituites - Lowers amount of other drug needed |
|
|
Routes of Admin Drugs
|
Nitrous Oxide - Inhalation
Nitroglycerin - Sublingual, dilates veins during angina to relieve hear workload Local Anesthetics - Subcutaneously Digoxin - Oral drug for congestive heart failure Fulvicin - Drug that speeds up due to fatty food Scopalamine - Anti-cholinergic that inhbiits motion sickness. Comes in a topical patch |
|
|
Protein Bumping Drugs
|
1) Ibuprofen and propofol binds heavily to albumin so when given to another albumin binding drug it bumps
2) Ibuprofen can bump warfarin causing lots of bleeding 3) Ibuprofen can bump anti-diabetes 2 drug Micronase. TOo much insulin release leads to hypoglycemia |
|
|
Liver Perfusion Drugs
|
1) Non-selective beta blockers - Reduce liver perfusion by (b1) inhibiting cardiac output and flow to the liver (b2)
2) Isoproterenol - Increase liver perfusion by stimulating beta receptor |
|
|
Biotransformation
|
1) CYP2E1 converts acetaminophen to inactive form and toxic NAPQI. NAPQI is hidnered by glutathione. Too much acetaminophen and glutathione is overwhelmed, NAPQI kills hepatocytes, and the result is bleeding
2) Acetylsalicycle acid T1/2 is 1 hour and it does pain management and inhibits inflammation. It's metabolite salicyclic acid has a T1/2 of 3 hours and only does pain managemnet. Taken together, dose at every 4 hours 3. Diazepam has a T1/2 of 24 hours, it's conjugate desmethyldiuazepam has a T1/2 of 12 hours, and it's conjugate oxazepam has a T1/2 of 6 hours |
|
|
Prodrugs
|
1) Codeine - Processed by CYP in SI to morphine
2) Ultram starts off as a anti-depressent that stimulates serotonin. It is de-methylated by CYP2D6 to a Mu Opioid |
|
|
CYP Contraindications
|
1) Grapefruit inhibits 3A4 so levels of lovastatin and simvastatin get too high leading to kidney problem
2) Don't take grapefruit juice or erythromycin before kids sedative midazolam 3) Don't mix cipro which inhibits CYP with caffeine substitute theophylline 4) Codeine and Ultram (2D6) levels stay high when surrounded by inhibitor like quinidine 5) Oral contraceptives don't work if given a 2C9 or 3A4 inducer which cuts down span of ethanol-estradiol. Examples are TB medicine rifampin and St John's Wort |
|
|
Iatrogenic Toxicity and Teratogen Testing
|
1) Corticosteroids - Too much can lead to bone loss
2) Metoclopramide - Leads to tardive dyskinesia Teratogen testing hard because it is species and strain specific.. 1) Aspirin cause problems in mouse but not human 2) Cortisone cause cleft palate in mouse ranging from 20% - 80% depending on the species |
|
|
CAST Drugs
|
Cardiac Arrythmia Suppression Trial - Section 7 of Nuremberg Code. Anti-arrhythmia drugs ended up doing more harm than placedo because they stopped PVC and caused death. Includes encainide, flecanide, and moricide
|
|
|
Potency Drugs
|
-Emax is the ceiling and represents efficacy
-Less dose to reach Emax is a more potent drug -Oxycodone (perks) and codeine have the same Emax but oxycodone are more potent |
|
|
Opioid Therapy
|
-Oxycodone is very addictive and has a K3 = 1, strong agonist. It binds the binding and active site of the receptor
-One option is to give a K3=0 antagonist like narcan which binds the binding site but not acitve -Another option to more slowly ease them off is to give a oxycodone analog buprenex which binds the binding site and only slightly binds the active site |
|
|
PNS Drugs
|
Muscarinic Cholinergic - Parasympathetic has agonist pilocarine and ACH. Antagonist are atropine and scopalamine
Alpha 1 - Agonist is NOR/EPI and antagonist is minipress and phentolamine (stop dental anesthesia) B1 - Agonist is EPI and antagonist is propranolol (non-selective) and metoprolol (B1 selective) Nicotinic M - Agonist is ACH and nicotine and antagonist is curare and succinylcholine |
|
|
Membrane Drugs
|
1) Nystatin - Punch holes in fungal cells and kills them
2) Local Anesthetics - Either block Na channel or expand membrane squeezing Na shut |
|
|
Enzyme Inhibitors
|
1) Anabolic Inhibitors - Prevent enzyme that converts substrate into active product. Example is aspirin which blocks COX-2 from making thromboxane A2
2) Catabolic Inhibit - Block enzyme so substrate build up has its effect. Physostigmine blocks cholinesterase so ACH build up and more muscle contraction. Nardil inhibits MAO which degrades NOR and serotonin so these build up |
|
|
Enzyme Stimulators
|
-EPI binds B-adrenergic leading to adenylate cyclase activation
|
|
|
Neurotransmitter Interaction
|
-Block or activate receptor NT bind to
Mimics - 1) pilocarpine - mimics ACH and binds M.C. BLocks 2) Atrophine - Blocks M.C.. Propranolol blocks betas Indirect - Allows NT to build up 1) Amphetamine help release NOR/DOPA so mood elevate and focus 2) Paxil and Prozac are seronton selective reuptake inhibitors so more sertonin 3) |
|
|
Anti-Cholinergics
|
-Refers to muscarinic cholinergic so parasympathetic blocks
-Leads to less saliva, less sweat, heart speeds up, constipation, dilated pupil A) Muscarinic Blockers 1) Belladona Alkaloids - Non-competitives 2) Teriatary Amine - Good lipid solubility 3) Quaternary Amines B) Ganglionic Blockers - Block all autonomic at nicotine N preganglionic C) Neuromuscular Blocker - Block nicotinic N but still anti-cholinergic |
|
|
Muscarinic Blockers
|
1) Belladona Alkaloids - Non-competitive blockers like atropine and scopalamine. Help with Myasthenia Gravis and Parkinsons. Don't use if glaucoma, C.A.D. asthma, GI blocked, Renal blocked
2) Tertiary Amines a) Anti-spasmodics which inhibit smooth muscle. Bentyl helps with IBS, dextro/ditropam help with urinary leakeg, and daricon helps with peptic ulcer b) Mydiatics - Help dilate the pupil. Cycolgyl and mydiacyl c) Anti-Parkinsons - Congenitin blocks DOPA all over body and benedryl is a anti-histamine 3) Quaternary Amines - Good at stopping gastric secretion. Robinul prevents bradycardia, and stops saliva and secretions like gastric and respiratory |
|
|
Ganglionic Blockers
|
-Block postsynaptic Nicotinic N all over the ANS. Can hinder both para and sym
1) Depolarizing - Activates the receptor and drains it, no depolarization. Includes nicotine, effects depend on system in charge 2) Non-depolarizing - Competes with ACH for nicotnic N receptor 1) Inversine - Good for hypertension. If withdrawal then replace with another hypertensive medicine 2) Afronad - Short acting and quick rebound good for hypertensive emergency. Not good for pregnancy. Take vasopressor like mephentermine or pehnylephrine if OD |
|
|
Neuromuscular Blocking Agents
|
-either depolarizing or non-depolarizing (competitive)
-Can be direct (at muscle) or indirect (in CNS) -Activated by antibiotic, analgesics, and quinidine -Ihibited by cholinergics, corticosteroids, and theophylline |
|
|
Depolarizers
|
1) Succinylcholine - Stimulation followed by paralysis. Metabolized by cholinesterase, Contraindications are low plasma pseudocholinesterase, malignant hyperthermia, and glaucoma. INteractis with any anti-cholinesterase like digitalis
2) Mylaxen - Inhibits cholinesteras to increase working time of succinylcholine |
|
|
Non-Depolarizer
|
1) Curare - reversible competitor antagonist of ACH causing temporary muscle paralysis
2) Turbocurare - Good for MYASTHENIA GRAVIS 3) Atracurium - Powerful non-depolarizers that doesn't release a lot of histamine 4) Doxacurium - Little histamine release 5) Flaxedil - No histamine release but less potent than turbocurare 6)Vencuronium - No histamine release |
|
|
Direct Acting Skeletal MUscle Relaxants
|
-Block release of Ca++ from sarcoplasm reticulum
-Affect fast acting muscles Dantrium - Taken orally for neurologic muscle spasm or IV for malignant hyperthermia |
|
|
Centrally Acting Skeletal Muscle Relaxant
|
-CNS depressor which relieve anxiety
-Fit problem in muscle tone due to descending otor tracks leading to jeriness, weakness, or bad dexterity 1) Liorseal - Activate GABA-B receptors to hyperpolarize cells so they don't release excitatory NT aspartate or glutamate 2) Valium - Stimulate GABA-a and allow in Cl- to hyperpolarize the cell 3) Methocarbamol is good for spasms and is a polysynaptic blocking drug |
|
|
Central Acting Skeletal Muscle Relaxant with Anti-Cholinesterase Property
|
-Include flexeril and norflex
|
|
|
Local Anesthetics
|
-Made of a aromatic lipid soluble group, a ester group which splits at first pass, and a amine which is water soluble so injectible
|
|
|
Locals - Esters
|
Novacaine and Procaine - Has a ester group that split to release allergen PABA so taken off the market
-These also had a high PKA so most of them were charged and didn't penetrate |
|
|
Methemhemoglobias
|
-Condition where strong oxider turn hemoglobin iron from Fe++ to Fe+++. Take methylene blue (reducer) as the antidote
1) Benzocaine - topical only 2) Prilocaine |
|
|
Local Details
|
-Different in carbon groups, amount of vasodilating, strength, longevity
-More carbons = more potent and more lipid soluble -Locals must cover 3 nodes of ranvier for effects -Either block NA channels or expand membrane 1) Mepivacaine - Good for people with heart condition 2) Prilocaine - Oxidizer, not a stront vasodilator, can cause paresthesia 3) Articaine/Septicaine - No ester split and very potent. Huge reports of paresthesia |
|
|
Dental Vasodilator
|
-Only two currently used are epinephrine and levonorephrine. EPI is weaker than alpha specific levono but there is less chance of hypertension with EPI since it's effects are distributed to the different receptors
|
|
|
Adrenergic Drugs Overview
|
-Stimulate alpha, beta, and dopamine receptors
-Can be direct acting at receptor, indirect acting through NT release or prevent reuptake, or both |
|
|
Adrenergic Roles
|
Alpha 1 - Vasoconstriction
Alpha 2 - Prevent presynaptic release of catecholamines Beta 1 - Increase myocardial contraction and cardiac output Beta 2 - vasodilate skeletal/liver/brain, bronchodilate, mydriasis, hyperglycemia, smooth muscle contraction like uterine |
|
|
Endogenous Catecholamines
|
Epinephrine - Great as a nasal decongestant, inhaled as a bronchodilator, and eye drop for open-angle glaucoma.
-Also good for cardiac arrest, shock, and prolonged locak Norepinephrine - Stimulates alpha and beta but especially alpha 1 for vasoconstriction. Good for hypotension but not shock and thrombosis. Enhanced by MAO inhibitors and TCA Dopamine - Target renal receptors to increase renal flow and the heart to increase contraction. At higher dose it targets alpha for vasoconstriction. Enhanced for MAO inhibitors and TCA |
|
|
Alpha Synthetic Catecholamines
|
Since it does vasocontriction it has a role in blood flow, nasal congestion, and glaucoma
Vasopressor - Phenylephrine increase BP via vasoconstriction and beta 1 heart stimulation Nasal Decongestant - Also phenylephrine constrict nasal vessel preventing congestion. If used too long can get nasal rebound 3) Opthalamic - Propine is converted to epinephrine by the liver. It can dilate the pupils for an exam or surgery or help remove/stop production of aqueous humor to treat open angle glaucoma |
|
|
Alpha 2 Synthetic Catecholamines
|
Catapress blocks catecholamine release on presynaptic terminal leading to hypotension, sedation, and analgesia
|
|
|
Beta Synthetic Catecholamines
|
Beta 1 - Dobutamine leads to increase heart contraction and cardiac flow without tachy problems of isoprotenerol
Beta 2 1) Bronchodilator - Albuterol - Helps relax bronchiole smooth muscle by stimulating adenylate cyclase. Good for asthma and COPD 2) Smooth Muscle - Use vasodilan and arlidin to vasodilate smooth muscle BV leading to peripheral vascular inefficiency treatment Beta 1 and Beta 2 Agonist 1) Isoproterenol - Good for asthma and cardiac arrest but can cause tachycardia 2) Epedrine - Stimulates alpha and beta. Trigger receptors and stimulate NE release |
|
|
CNS Stimulants and Anorexants
|
1) Phenylpropylamine - Amphentamine used as apatite suppresent, nasal decongestant, and ADHD. Caused strokes in young women so removed from the market
2) Sibutramine - Weight loss drug that prevent reuptake of serotonin, dopamine, and NE |
|
|
Adrenerigc Blocking Drugs
|
-Can be selective or non-selective for specific alpha or beta receptors. Can bind through competition or non-competition covalent bondign
|
|
|
Alpha Blockers
|
1) Nonselectives - Block alpha 1 on vascular smooth muscle leading to dilation and block alpha 2 at presynaptic terminal so more catecholamine release. Good for hypotension
a) Phentolamine - Competitive, short acting b) Dibenzyline - Noncompetitive and long acting. Good for hypotension and peripheral vascular disease Selectives 1) Minipress - Alpha 1 blocks for vasodilation and given to hypertensive patients 2) Aphrodyne - Alpha 2 block allows for catecholamine release, rpimarily NOR. Good for hypotension and sexual dysfunction |
|
|
Beta Blockers
|
-As you block the beta receptors more become available so withdrawal must be slloooowwww
a) Non-selective - Nadolol and proporanolol b) Selectives - Mostly selective for beta 1 but those for beta 2 are atenol and metoprolol |
|
|
Alpha and Beta Blockers
|
-Great to treat hypertension cause alpha 1 block vasodilates and beta 1 blocks cardiac contraction and reflex tachycardia
-Include carvedilol and labetalol |
|
|
Cholinergic Drugs
|
-Can be direct acting and bind to cholinergic receptor (nicotininc or muscarinic) but not both
-Can be indirect and inhibit cholinesterase, these act at muscarinic and nicotinic M I believe |
|
|
Direct Acting Cholinergics
|
Main one is nicotine. problem with figuring out nicotine effect on body is
1) Cigarettes contain many poisons, not just nicotin 2) Nicotin N receptor hard to predict since it's at the post-ganglionic receptor. Depending on system in charge it could have sympathetic or parasympathetic effect 3. Nicotine effect on the CNS is pleasure inducing leading to psychical and psychological dependence other direct acting drugs include acetylcholine, carbachol, and pilocarpine |
|
|
Indirect Acting Cholinergics
|
Physostigmine - At the muscarinic receptor it causes salivation and at the skeletal receptor it stimulates the muscle
Indirect Acting Drugs - Aricept, the stigmines, soman, sarin, tarcine |
|
|
Cholinergic Medical Treatments
|
1) Xerostomia - Give a cholinmimetric drug like pilocarine
2) Glaucoma - Give a drug that stimulates the ciliary muscle to release aqueous humor. Include pilocarpine, carbachol, and psychostigmine 3) Myasthenia Gravis - Antibody block muscarinic receptor so usually give a anticholinesterase like neostigmine 4) Alzheimers - Plaque in brain causes disruption. Found that also not enough ACH so give anticholinesterase like articept, stigmines, or tacrine. New drug is Namenda which blocks excitatory NT receptor. Gingko Bilboa also works 5) Nerve Gas - Tacrine, sarin, soman. To remove these from cholinesterase you can give pralidoxone 6) Urine Retention - Give cholinmimetric bethachol |
|
|
New Smoking Cessation Drugs
|
1) Wellbutrin - A anti-depresent that inhibit DA, 5-HT, or NOR reuptake
2) Straterra - Block reuptake of 5-HT and NOR. Used as a ADHD drug first 3) Revia - Opioid receptor antagonist that blocks pleasure that goes along with alcohol and drugs. Doesn't let people get high or enjoy 4) Chantix - Binds nicotine receptor in brain so less pleasure from smoking and less relapse |
