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NU578 - Unit 1 Questions and Answers
Schedule I - Correct Answer ✔✔Drugs in this schedule have no accepted medical use in the United States and have a high abuse potential. Examples are heroin, marijuana, LSD, peyote, etc. Schedule II - Correct Answer ✔✔Drugs in this schedule have a high abuse potential with severe psychic or physical dependence liability. Included are certain narcotic analgesics, stimulants, and depressant drugs. Examples are opium, morphine, codeine, hydromorphone, methadone, meperidine, oxycodone, anileridine, cocaine, amphetamine, methamphetamine, phenmetrazine, methylphenidate, amobarbital, pentobarbital, secobarbital, methaqualone, and phencyclidine. Schedule III - Correct Answer ✔✔Drugs in this schedule have an abuse potential less than those in Schedules I and II and include compounds containing limited quantities of certain narcotic analgesic drugs, and other drugs such as barbiturates, glutethimide, methyprylon, and chlorphentemine. Any suppository dosage form containing amobarbital, secobarbital, or pentobarbital is in this schedule. Schedule IV - Correct Answer ✔✔Drugs in this schedule have an abuse potential less than those listed in Schedule III and include such drugs as barbital, phenobarbital, chloral hydrate, ethchlorvynol, meprobabmate, chlordizepoxide, diazepam, oxazepam, chloroazepate, flurazepam, etc. Schedule V - Correct Answer ✔✔Drugs in this schedule have an abuse potential less than those listed in Schedule IV and consist primarily of preparations containing limited quantities of certain narcotic analgesic drugs used for antitussive and antidiarrheal purposes. Absorption - Correct Answer ✔✔Process of drug movement from its site of administration into the blood Most common mechanism for drug absorption - Correct Answer ✔✔passive diffusion First-pass effect (presystemic metabolism) - Correct Answer ✔✔Rapid hepatic inactivation of certain oral drugs
drug is metabolized (chemically altered) as it passes through either 1) gut wall, and
- liver. Distribution - Correct Answer ✔✔drug movement from the blood to the interstitial space of tissues and from there into cells Barriers to distribution - Correct Answer ✔✔- Blood brain barrier
- Placenta Physiologic Factors Affecting Distribution - Correct Answer ✔✔- Perfusion
- Binding of drug to plasma protein
- Specialized Distribution Barriers Albumin - Correct Answer ✔✔Binds acidic drugs Protein (albumin) binding - Correct Answer ✔✔Prevents bound drug molecules from leaving the bloodstream Prolongs the distribution phase (Increases half-life) alpha-1 acid glycoprotein - Correct Answer ✔✔Binds basic drugs Reservoir effect - Correct Answer ✔✔ Blood-Brain Barrier (BBB) - Correct Answer ✔✔no intercellular pores between brain capillary endothelial membranes due to the presence of tight junctions between cells To gain access to the brain from the capillaries, drugs must - Correct Answer ✔✔1) diffuse across cells (lipid-soluble, nonionized form) or
- or be actively transported by a carrier Placental Barrier - Correct Answer ✔✔Transfer of drugs is relatively slow with the equilibration time between maternal blood and fetal tissues estimated at about 15 minutes for some drugs and almost an hour for other drugs. (Virtually every drug used for therapeutic purposes can and does cross the placenta.)
ex: fosphenytoin --> Codeine Phase II (synthetic) reactions - Correct Answer ✔✔occur in the liver and gut wall. conjugated metabolites - Correct Answer ✔✔virtually always inactive, very polar and/or ionized, and easily excreted. (products of Phase II reactions) Enterohepatic circulation & cycling - Correct Answer ✔✔Repeating cycle in which a drug is transported from the liver into the duodenum (via bile duct) and then back to the liver (via portal blood) Limited to drugs that have undergone glucuronidation Induction of the CYP isoenzymes - Correct Answer ✔✔Increase rate of drug metabolism (Lowers drug level) Inhibition of CYP isoenzymes - Correct Answer ✔✔Decrease rate of drug metabolism (Increases drug level) grapefruit juice - Correct Answer ✔✔Effects GI CYP3A isozyme decreasing intestinal metabolism of many drugs (Effects persist up to 3 days after last glass of juice!) Drugs affected by grapefruit juice - Correct Answer ✔✔- Statins
- Antihistamines
- Calcium channel blockers
- Psychiatric drugs
- Immunosuppressants
- Methadone
- Viagra
- saquinavir (Invirase)
- amiodarone (Cordarone)
- Caffeine Empty stomach - Correct Answer ✔✔Administer at least 1 hour before or 2 hours after a meal Excretion - Correct Answer ✔✔removal of a drug from the body Glomerular filtration - Correct Answer ✔✔Drugs are moved from blood into tubular urine passive tubular reabsorption - Correct Answer ✔✔drugs that are lipid-soluble undergo passive reabsorption from the tubule back into the blood active tubular secretion. - Correct Answer ✔✔large, charged drug molecules added to the urine for excretion from the body. Non-Renal Routes of Excretion - Correct Answer ✔✔breast milk, bile, lungs, sweat, saliva Factors that affect renal drug excretion - Correct Answer ✔✔pH-dependent ionization Competition for active tubular transport Age P-Glycoprotein - Correct Answer ✔✔transmembrane protein that transports drugs out of cells Pumps drugs out of organs for elimination and excretion P-Glycoprotein induction - Correct Answer ✔✔decreased absorption, fetal drug exposure, & brain/CNS drug exposure increased drug elimination Drugs to avoid in pregnancy - Correct Answer ✔✔- Antiseizure Drugs
- Nitrofurantoin, sulfonamides, tetracyclines
- ACEI, ARBs
- Lithium
- NSAIDs
- Warfarin
- Oral hypoglycemics
Can act as an agonist and an antagonist therapeutic index - Correct Answer ✔✔ratio of LD50 to ED The higher the therapeutic index, the safer the drug LD50 = Dose that is lethal to 50% of population ED50 = Dose that produces therapeutic effect in 50% of population Pharmacogenomics - Correct Answer ✔✔The study of how genetic variations affect individual responses to drugs Autonomic Nervous System - Correct Answer ✔✔controls cardiac & smooth muscles, & glandular secretion Sympathetic: - Correct Answer ✔✔"fight-or-flight" Regulates cardiovascular system Temperature Parasympathetic: - Correct Answer ✔✔"rest & digest" SLows HR Increased gastric secretion Empty bladder & bowel Focus eyes Constrict pupils Contract bronchial smooth muscle Peripheral Nervous System Neurotransmitters - Correct Answer ✔✔Acetylcholine, norepinephrine, epinephrine cholinergic receptors - Correct Answer ✔✔receptors that mediate responses to acetylcholine adrenergic receptors - Correct Answer ✔✔receptor sites for the sympathetic neurotransmitters norepinephrine and epinephrine types of cholinergic receptors - Correct Answer ✔✔nicotinic and muscarinic
types of adrenergic receptors - Correct Answer ✔✔alpha 1, alpha 2, beta 1, beta 2 Αlpha 1 - Correct Answer ✔✔Vasoconstriction ↓secretions pupil dilation ↓GI motility urinary retention alpha 1 agonists uses - Correct Answer ✔✔Vasoconstriction: Nasal decongestion Adjunct to anesthesia Increase BP Mydriasis: Pupil dilation for exam/surgery Adverse effects of alpha 1 agonists - Correct Answer ✔✔HTN Necrosis Bradycardia Alpha 2 - Correct Answer ✔✔CNS sympathetic outflow (postsynaptic) ↓NE release (presynaptic) ↓insulin release Alpha 2 agonist uses - Correct Answer ✔✔Reduction of sympathetic outflow fo heart and vessels Relief of severe pain Beta 1 - Correct Answer ✔✔↑HR, CO, automaticity, contractility, ↑renin secretion Beta 1 agonist uses - Correct Answer ✔✔Heart failure Shock AV heart block Cardiac arrest Adverse effects of beta 1 agonists - Correct Answer ✔✔tachycardia
Dopamine (Intropin) - Correct Answer ✔✔Acts on dopamine --> beta1 --> and alpha1 (dose dependent receptor specificity) Low doses maintain good renal blood flow, higher doses increase BP ↑ cardiac contractility Used for shock Dobutamine (Dobutrex) - Correct Answer ✔✔Works on Beta 1 receptors ↑HR, contractility Used for cardiac stimulation in HF Isoproterenol - Correct Answer ✔✔Beta-selective adrenergic agonist Used for AV heart block, cardiac arrest Phenylephrine (NeoSynephrine) - Correct Answer ✔✔Works on alpha 1 receptors vasoconstriction Used in cold meds Elevates BP Also used to dilate pupil Albuterol (Ventolin) - Correct Answer ✔✔Works on Beta2 receptors bronchiolar and uterine relaxation Used to prevent asthma; Others used for premature labor Amphetamines (d-Amphetamine) - Correct Answer ✔✔Heightened mood, decreased appetite
Used for ADD and narcolepsy Pseudoephedrine (Sudafed) - Correct Answer ✔✔Works on alpha 1 receptors Vasoconstriction Used for nasal congestion Phenoxybenzamine (Dibenzyline) - Correct Answer ✔✔Blocks alpha 1, alpha 2 receptors; Vasodilation used for Pheochromocytoma Long-acting, po q day Dosing Phentolamine (Regitine) - Correct Answer ✔✔Blocks alpha 1, alpha 2 receptors; Vasodilation Used for diagnosis of pheochromocytoma and to reduce necrosis from extravasation of drugs Adverse effects of alpha 1 blockers - Correct Answer ✔✔Orthostatic hypotension Reflex tachycardia Congestion Inhibition of ejaculation Sodium retention Adverse effects of Alpha 2 blockers - Correct Answer ✔✔reflex tachycardia Adverse effects of beta 1 blockers - Correct Answer ✔✔BRadycardia Decreased CO Heart Failure AV HEart block Rebound Cardiac excitation Adverse effects of beta 2 blockers - Correct Answer ✔✔bronchoconstriction Hypoglycemia Prazosin (Minipress) - Correct Answer ✔✔selective alpha 1 blocker
Ophthalmic also used to ↓ HR Metoprolol (Lopressor) Atenolol (Tenormin) Acebutolol (Sectral) Esmolol (Brevibloc) - Correct Answer ✔✔Beta 1 Specific Used for HTN (less bronchospasm) Indirect alpha blockers - Correct Answer ✔✔Used for: HTN Severe pain ADD Clonidine (Catapres) - Correct Answer ✔✔centrally acting alpha 2 agonist Used for HTN Cevimeline (Evoxac) - Correct Answer ✔✔muscarinic agonist Used for dry mouth in Sjogren's Do not use in asthma Pilocarpine (Pilocar, OcusertPilo) - Correct Answer ✔✔muscarinic agonist used for Glaucoma; oral Tx for Sjogren's Nicotinic-N receptors - Correct Answer ✔✔located in Ganglia Promote release of epinephrine from adrenal medula
Nicotinic-M receptors - Correct Answer ✔✔causes skeletal muscle contraction muscarinic - Correct Answer ✔✔located in organs Sites of muscarinic receptors - Correct Answer ✔✔Eye - Focus & dilate pupil Heart - decreased HR Lung - Bronchial constriction, secretions Bladder - Voiding of bladder GI Tract - Salivation, secretions, motility, defectaion Sweat Glands Sex Organs - Erection Blood Vessels - Vasodilation Bethanechol (Urecholine) - Correct Answer ✔✔muscarinic agonist Used for Urinary retention, GI atony, ileus Contraindicated for bladder obstruction, GI obstruction, & hyperthyroidism Treatment of muscarinic poisoning - Correct Answer ✔✔Atropine Mirabegron - Correct Answer ✔✔OAB drug, works on beta3 receptors *NOT anticholinergic Cholinesterase inhibitors - Correct Answer ✔✔Prevent enzymatic breakdown of acetylcholine at nerve endings, thus allowing accumulation of the neurotransmitter Improve strength of contraction in all muscles including respiratory Neostygmine (Bloxiverz) - Correct Answer ✔✔Cholinesterase inhibitor Treatment of myasthenia gravis Reverse non-depolarizing neuromuscular blockade after surgery Organophospates - Correct Answer ✔✔Irreversible cholinesterase inhibitors Highly toxic
incontinence, ER codes Scopolamine (Transdermscop) - Correct Answer ✔✔ACh antagonist (anticholinergic) Used for motion sickness Dicyclomine (Bentyl) - Correct Answer ✔✔ACh antagonist Used fro irritable bowel Trihexyphenidyl (Artane) Benztropine (Cogentin) - Correct Answer ✔✔ACh antagonist Used for parkinson's disease Treatment of anticholinergic (antimuscarinic) poisoning - Correct Answer ✔✔physostigmine *activated charcoal also used to decrease intestinal absorption Darifenacin (Enablex) Oxybutyinin (Ditropan) Solifenacin (VESIcare) Tolteridine (Detrol) Trospium (Sanctura) Fesoterodine (Toviaz) - Correct Answer ✔✔Anticholinergic Block muscarinic receptors on the bladder detrusor muscle Used for overactive bladder Succinylcholine (Anectine) - Correct Answer ✔✔Depolarizing neuromuscular blocker Specific for ACh on skeletal muscle Onset within 30 seconds
to 1 minute, duration of action about 5 minutes. Used primarily to facilitate intubation or for endoscopy. Non-depolarizing (competitive) neuromuscular blockers - Correct Answer ✔✔compete with acetylcholine for binding to Nicotinic-M recepotors Cause skeletal muscle paralysis ** Do not reduce consciousness of perception of pain Curare Family: (Atracurium Cisatracurium Pancuronium Rocuronium Vecuronium) - Correct Answer ✔✔Nondepolarizing neuromuscular blocker Specific for ACh on skeletal muscle All work for about 20-40 min; recovery may take an hour, given IV Used for longer surgical procedures, as adjuncts to anesthesia. ***Watch for Malignant Hyperthermia as a side effect: Malignant Hyperthermia - Correct Answer ✔✔presents as muscle rigidity, tremors, and high fever soon after exposure to these agents. Treatment is to d/c the
Curare - muscle relaxant pH partitioning Ion Trapping - Correct Answer ✔✔Drugs accumulate on the side of membrane that favors ionization ex: acidic drugs will accumulate on the alkaline side Factors affecting absorption - Correct Answer ✔✔rate of dissolution surface area blood flow lipid solubility pH partitioning Barriers to PO absorption - Correct Answer ✔✔Epithelial cells Capillary walls Sometimes p-glycoprotein Factors affecting PO absorption - Correct Answer ✔✔Solubility & stability Gastric.intestinal pH Gastric emptying time Food in the gut Coadministration of other drugs Coatings on the drug Abscesses & tumors - Correct Answer ✔✔Low regional blood flow affects therapy (Lack of blood flow inhibits drug delivery to the site. Abscess - Pus-filled pockets don't have internal blood vessels Solid tumors - have a limited blood supply) Idiosyncratic effect - Correct Answer ✔✔an uncommon drug response resulting from a genetic predisposition ex: G6PD deficiency
Paradoxical effect - Correct Answer ✔✔a response to a medication that is the opposite of what is expected iatrogenic disease - Correct Answer ✔✔disease produced by drugs physical dependence - Correct Answer ✔✔a state in which the body has adapted to drug exposure in such a way that an abstinence syndrome will result if drug use is discontinued carcinogenic effect - Correct Answer ✔✔the ability of certain medications and environmental chemicals to cause cancers teratogenic effect - Correct Answer ✔✔causal relationship between the drug use of a mother and congenital abnormalities (congenital defect) Hepatotoxic drugs - Correct Answer ✔✔as some drugs undergo metabolism by the liver, they are converted to toxic products that can injure liver cells LFTs to assess liver function and hepatotoxicity - Correct Answer ✔✔AST & ALT QT Interval Drugs - Correct Answer ✔✔the ability of some medications to prolong the QT interval on the electrocardiogram, thereby creating a risk of serious dysrhythmias Patient at risk for adverse effects of QT drugs - Correct Answer ✔✔- Older adults
- Patients with dysrhythmias
- Low K and Mag
- Women
- Current use of other QT drugs pharmacodynamic tolerance - Correct Answer ✔✔adaptive changes in systems affected by the drug so that the response to a given concentration of drug is reduced metabolic tolerance - Correct Answer ✔✔Accelerated rate of drug metabolism Tachyphylaxis - Correct Answer ✔✔Reduction in drug responsiveness brought on by repeated dosing over a short time ex: transdermal nitro
