PHARMACOLOGY EXAM 1 STUDY GUIDETEST EXAM WITH 208QUESTIONS AND ANSWERS ALL ANSWERS GUARANT, Exams of Nursing

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What enzyme mediates the majority of phase 1 drug biotransformations? - CORRECT ANSWERS Heme Protein Cytochrome P- True or False: phase 1 drug biotransformations have high substrate specificity and fast reaction kinetics. - CORRECT ANSWERS False Oxidation is considered a phase ____ reaction. Name an example. - CORRECT ANSWERS 1. 1

2. Acetanilid -> acetaminophen True or False: Epoxidation is considered a phase 1 reaction. - CORRECT ANSWERS True Demethylation is considered a phase ____ reaction. Name an example - CORRECT ANSWERS 1. 1
3. Codeine -> Morphine Reduction is considered a phase ____ reaction. - CORRECT ANSWERS 1 Dehalogenation is considered a phase ____ reaction. - CORRECT ANSWERS 1 Which phase 1 drug biotransformation tends to affect esters and amides? - CORRECT ANSWERS Hydrolysis

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Deacetylation is considered a phase ____ reaction. Name two examples. - CORRECT ANSWERS 1. 1

2. Aspirin -> salicylic acid AND Heroin -> Morphine Glucuronidation is considered a phase ____ reaction, and mainly affects _____ and ______ groups. - CORRECT ANSWERS 1. 2
3. hydroxyl and carboxyl Sulfation is considered a phase ____ reaction and tends to occur at _________ (high/low) drug concentrations. - CORRECT ANSWERS 1. 2
4. low Glutathionation is considered a phase ____ reaction. - CORRECT ANSWERS 2 What is a consequence of a patient with a defective N-acetyl cysteine? - CORRECT ANSWERS Liver cell death may occur if the patient takes a high dose of acetaminophen. Which age groups have the lowest hepatic drug conjugation activity? - CORRECT ANSWERS Infants and elderly True or False: both diet and genetics can affect drug metabolism. - CORRECT ANSWERS True

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What is the clearance rate of a drug that is excreted through glomerular filtration?

• CORRECT ANSWERS 125 mL / minute True or False: drugs that are excreted through glomerular filtration undergo passive filtration, allowing only free drugs to pass. - CORRECT ANSWERS True How are protein bound drugs secreted in the kidneys? - CORRECT ANSWERS Active tubular secretion into the nephron What type of metabolites tend to undergo biliary secretion? - CORRECT ANSWERS

1. Glucuronides
2. High MW conjugates A drug is being recycled through hepatic recycling. What may be administered to the patient to disrupt it? - CORRECT ANSWERS Charcoal True or False: most drugs undergo hydrolysis as a phase 1 reaction. - CORRECT ANSWERS False; oxidation. True or False: the goal of phase 2 metabolism is to conjugate large non-polar molecules for excretion. - CORRECT ANSWERS False; polar. What is the major route of drug excretion? - CORRECT ANSWERS Renal

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A _____ order reaction occurs below the Lm and has a linear relationship with regards to concentration and rate of catalysis. - CORRECT ANSWERS first A ______ order reaction occurs above the Km and rate is insensitive to the drug concentration. - CORRECT ANSWERS zero True or False: the majority of drugs undergo zero order catalysis. - CORRECT ANSWERS False; first. What is K(el)? - CORRECT ANSWERS Proportionality constant that describes the fraction of drug eliminated per unit of time. The concentration of a drug (y) is plotted against time (x). The graph produced an exponential decay. What type of elimination is described by the graph? - CORRECT ANSWERS First order How can you find the Kel of a first order reaction? - CORRECT ANSWERS 1. Plot concentration against time (exponential decay).

2. Take the natural log -> produces straight line.
3. Take the slope of the line. What is the half-life? - CORRECT ANSWERS The time for drug concentration to fall by 50%. What is the formula for half-life? - CORRECT ANSWERS half life = .693 / K(el)

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What is the formula for Kel? - CORRECT ANSWERS Kel = .693 / half-life What is the volume of distribution? Formula? - CORRECT ANSWERS 1. Measures drug distribution between the plasma and rest of the body.

2. Vd = initial dose / concentration (time 0) True or False: in a first order reaction, you can double the effectiveness of the drug by doubling the dose. - CORRECT ANSWERS False; doubling the dose will only increase the duration by 1 half life. The concentration of a drug (y) is plotted against time (x). The graph produced a straight line. What type of elimination is described by the graph? - CORRECT ANSWERS zero-order True or False: in zero order elimination, the time it takes for blood level of the drug to drop below an arbitrary level is directly proportional to the amount ingested. - CORRECT ANSWERS True ___________ occurs when the rate of drug infusion is equal to the rate of drug elimination. - CORRECT ANSWERS Steady-state For a first-order reaction to reach plateau, it takes ________ half lives. - CORRECT ANSWERS 5 (96.9%)

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True or False: the plateau principle can be used to determine the concentration that steady-state occurs. - CORRECT ANSWERS False; just the time it takes to reach steady state. What is a loading dose? Formula? - CORRECT ANSWERS 1. An initial dose that is larger than the maintenance dose that's used to quickly reached the therapeutic dose.

2. Loading dose = Vd x Concentration (at steady state) What is the formula for clearance? - CORRECT ANSWERS Cl = K(el) x Vd Drug clearance is dominated by the _______ and ________. - CORRECT ANSWERS liver and kidneys What is the formula for maintenance dose? - CORRECT ANSWERS Maintenance dose = clearance x concentration (at steady state) True or False: patients should be given small maintenance doses in order to prevent large spikes in drug concentration. - CORRECT ANSWERS True True or False: sympathetic nerves arise from the cervical and thoracic regions of the spinal cord. - CORRECT ANSWERS False; thoracic and lumbar 1. True or False: sympathetic nerves have a long pre-ganglion and short post- ganglion. - CORRECT ANSWERS False

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Parasympathetic nerves arise from __________. - CORRECT ANSWERS brain stem What is the neurotransmitter and receptor used by somatic nervous system? - CORRECT ANSWERS 1. neurotransmitter = acetylcholine

2. receptor = nicotinic What is the neurotransmitter and receptor used by parasympathetic nervous system? - CORRECT ANSWERS 1. Neurotransmitters = acetylcholine
3. Receptors = nicotinic (pre-ganglion) and muscarinic (post-ganglion) What is the neurotransmitter and receptor used by sympathetic nervous system? - CORRECT ANSWERS 1. Neurotransmitter = acetylcholine (pre-ganglion) and norepinephrine (post-ganglion)
4. Receptors = nicotinic (pre-ganglion) and adrenergic (post-ganglion) Nicotinic receptors are _________. - CORRECT ANSWERS ligand-gated channels True or False: muscarinic receptors are ligand-gated channels. - CORRECT ANSWERS False; g-protein. Acetylcholine is inactivated through __________. - CORRECT ANSWERS acetylcholinesterase

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Name two cholinergic drugs that are nicotinic ganglionic stimulants. - CORRECT ANSWERS 1. nicotine

2. varenicline Cholinergic drugs that are nicotinic receptor antagonists are used to treat __________. - CORRECT ANSWERS hypertension Name three cholinergic drugs that are used as nicotinic ganglionic antagonists. - CORRECT ANSWERS 1. Mecamylamine
3. Hexamethonium
4. Trimethaphanm ___________ is a cholinergic muscarinic agonist used to stimulate salivation. - CORRECT ANSWERS Pilocarpine ____________ is a cholinergic muscarinic agonist used to treat asthma. - CORRECT ANSWERS Methacholine ___________ is a cholinergic muscarinic agonist used in eye surgery. - CORRECT ANSWERS Acetylcholine ______________ is a cholinergic muscarinic antagonist used to induce pupil dilation. - CORRECT ANSWERS Atropine, scopolamine

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______________ is a cholinergic muscarinic antagonist used to induce bronchial dilation. - CORRECT ANSWERS Ipratropium What type of drug may be used to decrease salivation during oral surgery? - CORRECT ANSWERS Anti-muscarinics What is the purpose of cholinesterase inhibitors? - CORRECT ANSWERS Blocks the enzyme cholinesterase to prolong the duration of acetylcholine in the synapse. What type of drug is physostigmine/neostigmine? And what are they used to treat? - CORRECT ANSWERS 1. Cholinesterase inhibitors

2. Myasthenia gravis - autoimmune disease associated with destruction of ACh receptors on muscles. True or False: adrenergic receptors are G protein coupled receptors. - CORRECT ANSWERS True Name some effects of the alpha-1 adrenergic receptors. - CORRECT ANSWERS 1. vasoconstriction
3. increased blood pressure
4. closure of bladder sphincters Name some effects of the alpha-2 adrenergic receptors. - CORRECT ANSWERS 1. inhibition of NE release

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2. inhibition of ACh release
3. inhibition of insulin release What neurotransmitter most commonly binds to alpha-1 adrenergic receptors? - CORRECT ANSWERS Norepinephrine Name some effects of the beta-1 adrenergic receptors. - CORRECT ANSWERS 1. increased heart rate
4. increased mycardial activity
5. increased renin Name some effects of the beta-2 adrenergic receptors. - CORRECT ANSWERS 1. bronchodilation
6. vasodilation How are catecholamines cleared from the synaspe? - CORRECT ANSWERS Reuptake Describe the mechanism of sympathomimetics. - CORRECT ANSWERS 1. Act as receptor agonists.
7. Increase catecholamine release.
8. Decrease catecholamine reuptake. Name two agonists of alpha-1 receptors. - CORRECT ANSWERS 1. Norepinephrine

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2. Phenylephrine Name two antagonists of alpha-1 receptors. - CORRECT ANSWERS 1. Phentolamine
3. Prazosin Name an agonist of Beta-1 receptors. - CORRECT ANSWERS Isoproterenol Name two beta antagonists. - CORRECT ANSWERS 1. Propanolol
4. Metoprolol Name an agonist of beta-2 receptor. - CORRECT ANSWERS Albuterol ____________ is a non-selective adrenergic agonist used to treat anaphylaxis. - CORRECT ANSWERS Epinephrine __________ is a non-selective adrenergic agonist used to increase blood pressure.

• CORRECT ANSWERS Norepinephrine _________ is an adrenergic agonist that is selective for alpha-1 receptor and used to increase blood. - CORRECT ANSWERS Phenylepherine __________ is an adrenergic agonist that is non-selective for B receptors and increases heart rate and induces vasodilation. - CORRECT ANSWERS Isoproterenol

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___________ is an adrenergic agonist that is selective for beta-2 receptors and induces bronchodilation. - CORRECT ANSWERS Albuterol ___________ is an adrenergic antagonist that is non-selective for alpha receptors and is used to treat hypertension. - CORRECT ANSWERS Phentoalmine ___________ is an adrenergic antagonist that is selective for alpha-1 receptors and is used to treat hypertension. - CORRECT ANSWERS Prazosin ___________ is a non-selective B adrenergic antagonist that is used to decrease blood pressure and increases airway resistance. - CORRECT ANSWERS Propanolol ___________ is a selective Beta-1 adrenergic antagonist that is used to decrease blood pressure with no effect on airway resistance. - CORRECT ANSWERS Metoprolol An __________ drug is used to treat chronic anxiety. - CORRECT ANSWERS anxiolytic A __________ drug decreases activity, moderates excitement and calms the patient. - CORRECT ANSWERS sedative A _____________ drug produces drowsiness and facilitates the onset and maintenance of sleep. - CORRECT ANSWERS hypnotic

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Which CNS depressants have a narrow margin of safety and a linear dose response curve? - CORRECT ANSWERS Barbiturates, alcohol, chloral hydrate and GHB. Which CNS depressants have a flat dose response curve and a greater margin of safety? - CORRECT ANSWERS Benzodiazepines True or False: barbiturates are most commonly used as anxiolytics. - CORRECT ANSWERS False, BDZs. Describe the mechanism of action of GABA neurotransmitters. - CORRECT ANSWERS 1. GABA is released from the inhibitory synapse and binds to GABA receptors.

2. GABA receptors are ligand gated channels that permit chloride ions to move through.
3. Chloride hyperpolarizes the cell and prevent action potentials from generating. How do benzodiazepines affect GABA receptors? - CORRECT ANSWERS Increase the affinity of GABA for the receptor -> more chloride passes through.

• cannot open receptor on its own! How do barbiturates affect GABA receptors? - CORRECT ANSWERS Increase the GABA receptor opening time so more chloride passes through
• can open receptor on its own!

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Which drug is more potent: barbiturates or benzodiazepines? - CORRECT ANSWERS Benzodiazepines True or False: BDZs increase the potency of a receptor while BARBs increase the efficacy and potency. - CORRECT ANSWERS True Benzodiazepines have high lipid solubility, which allows for rapid entry into the _____. They are metabolized by the _________. - CORRECT ANSWERS 1. CNS

2. liver True or False: benzodiazepines and barbiturates may break down into metabolites that are metabolically active. - CORRECT ANSWERS False; only benzodiazepines. Name two benzodiazepines that are directly metabolized to glucuronides and have less residual effects. - CORRECT ANSWERS Lorazepam and Oxazepam ___________ is a benzodiazepine that is given intravenously only and commonly used as an adjunct to anesthesia during surgery. - CORRECT ANSWERS Midazolam ___________ is a long-acting benzodiazepine with a half life of 20-50 hours. It's commonly used during long-flights. - CORRECT ANSWERS Diazepines. ___________ is a short-acting benzodiazepine with a half life of 1.5-5 hours. It's commonly used as a sleep aid. - CORRECT ANSWERS Triazolam

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What CNS depressant is used as an anticonvulsant to treat epilepsy and alcohol withdrawal? - CORRECT ANSWERS Diazepam Name 5 side effects of benzodiazepines. - CORRECT ANSWERS 1. respiratory depression

2. euphoria
3. paradoxical excitement
4. amnesia
5. withdrawal True or False: a benzodiazepine combined with alcohol produces additive effects and may lead to a lethal dose very quickly. - CORRECT ANSWERS True For CNS depressants, giving ___________ before _________ may induce faster metabolism due to induction of P450 enzymes; however, the opposite will have no affect on metabolism. - CORRECT ANSWERS 1. barbiturates
6. benzodiazepines _____________ is a benzodiazepine antagonist that may be given to patients intravenously that have succumb to a coma from combination of benzodiazepines and alcohol. - CORRECT ANSWERS Flumazenil Which barbiturate is used as an ultra-short acting anesthetic? - CORRECT ANSWERS Thiopental

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Which barbiturate is commonly used as a sedative? - CORRECT ANSWERS Pentobarbital What is the indication for phenobarbital? - CORRECT ANSWERS Treating patients with epilepsy. A patient is at high risk for seizures due to reaction with local anesthetics. What CNS depressant may be given prior to surgery to reduce this response? - CORRECT ANSWERS Midazolam What CNS depressant is given to patients to suppress the gag reflex? - CORRECT ANSWERS Diazepam Name two drugs that can be used as CNS active muscle relaxants. - CORRECT ANSWERS Mephensin and Methocarbamol _________ is a tricyclic antidepressant that may be used as a non-sedating muscle relaxant, but has anticholinergic affects. - CORRECT ANSWERS Cyclobenzaprine What is hydroxzine? - CORRECT ANSWERS Antihistamine that may be used as a non-depressant sedative/hypnotic. What is diphenhydramine? - CORRECT ANSWERS Antihistamine that may be used as a non-depressant sedative/hypnotic.

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__________ is a non-sedating anxiolytic that is a partial serotonin agonist that promotes presynaptic release of serotonin. - CORRECT ANSWERS Buspar Name 4 non-sedating anxiolytics. - CORRECT ANSWERS 1. Buspar

2. Propanolol (B blocker)
3. Clonidine (alpha 2 agonist)
4. tricyclic antidepressants ___________ is a cheap sedative often used for pediatric patients. - CORRECT ANSWERS Chloral hydrate ___________ is a benzodiazepine that is often used to treat panic disorder and agorophobia. - CORRECT ANSWERS Alprazolam What type of drug is flurazepam? - CORRECT ANSWERS Benzodiazepine Describe the mechanism of NSAID activity on COX enzymes. - CORRECT ANSWERS NSAIDs inhibit COX in the production of PGG2 and POX in the production of PGH2. Which COX enzyme is mainly involved in inflammatory responses, fever, and algesia, and constitutively expressed in the blood vessels? - CORRECT ANSWERS COX-

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What is the most abundant prostanoid? - CORRECT ANSWERS PGE Describe how NSAIDs can reduce inflammation. - CORRECT ANSWERS NSAIDs inhibit the production of inflammatory mediators (prostaglandins, IL, chemokines, histamine) through inhibition of COX-2 enzymes. True or False: the anti-inflammatory effects of NSAIDs require much higher doses than analgesic and antipyretic effects. - CORRECT ANSWERS True Describe how NSAIDs can reduce pain sensation. - CORRECT ANSWERS 1. COX produces PGE

2. PGE2 acts on EP receptors to produce PKA
3. PKA phosphorylates TRPV1 receptors and makes it more sensitive.
4. NSAIDs block this process through COX inhibition. Describe how NSAIDs can reduce elevated body temperature. - CORRECT ANSWERS 1. COX-2 produces PGE
5. PGE2 acts in the hypothalamus to increase body temperature.
6. NSAIDs inhibit COX production Describe how NSAIDs can reduce clotting. - CORRECT ANSWERS 1. COX- produces TxA2 (platelets).
7. TxA2 mediates vasoconstriction and platelet aggreagation.
8. NSAIDs block COX-

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True or False: COX-2 promotes clotting and platelet aggregation through production of prostaglandins. - CORRECT ANSWERS False; inhibit platelet aggregation. __________ covalently modifies and irreversible inhibits platelet COX-1 and prevents thrombosis; however, ________ may bind irreversibly to COX-1 and prevent inhibition of COX-1. - CORRECT ANSWERS 1. Aspirin

2. ibuprofen How do NSAIDs affect the renal system? - CORRECT ANSWERS 1. COX enzymes produce prostanoids.
3. Prostanoids may increase or decrease sodium retention (mainly decrease).
4. NSAIDs promote sodium retention -> increase blood pressure.

• NSAIDs also decrease blood flow to the kidneys! How do NSAIDs affect the GI system? - CORRECT ANSWERS 1. COX-1 generates PGE2.

2. PGE2 inhibits stomach acid secretion, increases mucosal blood flow, and promotes mucus secretion.
3. NSAIDs inhibit COX leading to GI distress, gastric ulcers and acute hemorrhage. Which COX enzyme plays a role in wound healing and initiation/progression of labor? - CORRECT ANSWERS COX-

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Aspirin irreversibly inhibits COX via ________. - CORRECT ANSWERS acetylation of active site serine True or False: Aspirin is rapidly converted to salicylate, which undergoes zero- order metabolism. - CORRECT ANSWERS True _________ and _______ are two non-selective COX inhibitors that do not contain salicylate. - CORRECT ANSWERS Ibuprofen and naproxen ___________ is a selective COX-2 inhibitor (no COX-1 side effects); however, may lead to increased blood pressure, increased oxidative stress and inhibition of anti- thrombogenic prostaglandins. - CORRECT ANSWERS Celecoxib Name 2 effects of acetaminophen. - CORRECT ANSWERS 1. anti-pyretic

2. analgesic True or False: acetaminophen does not have anti-inflammatory effects. - CORRECT ANSWERS True ___________ can be administered to patients overdosing on acetaminophen. - CORRECT ANSWERS Acetylcysteine What is an opiate? - CORRECT ANSWERS Drug derived from opium poppy - morphine, codeine, thebaine.

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Opioid receptors are in the ______ superfamily and are coupled to ___________ proteins. - CORRECT ANSWERS 1. GPCR

2. inhibitory G Which opioid receptor binds the majority of opioid drugs and mediates spinal/supraspinal analgesia, respiratory depression, euphoria, sedation, miosis and GI effects? - CORRECT ANSWERS Mu Which opioid receptor is responsible for spinal cord mediated analgesia and dysphoria? - CORRECT ANSWERS Kappa Which opioid receptor plays a role in the development of tolerance? - CORRECT ANSWERS Delta Which endogenous opioid peptides bind to mu receptors? - CORRECT ANSWERS B-endorphins, endomorphins, and semi binds to enkephalins and dynorphins. Which endogenous opioid peptides bind to kappa receptors? - CORRECT ANSWERS dynorphins Which endogenous opioid peptides bind to delta receptors? - CORRECT ANSWERS Enkephalins and semi binds to B-endorphins. What is principal therapeutic effect of opioids? - CORRECT ANSWERS Analgesia without loss of conciousness

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Opioids reduce both the __________ and __________ components of pain. - CORRECT ANSWERS sensory and emotional True or False: opioids most effectively reduce sharp pain sensation. - CORRECT ANSWERS False; dull. Describe the ascending pain transmission pathway. Where does modulation occur? - CORRECT ANSWERS 1. Sensory nerve -> Dorsal root ganglion -> dorsal horn -> parabrachial nuclei -> thalamus -> cortex

2. Modulated at the DRG, dorsal horn, parabrachial nuclei, and thalamus. Describe the descending pain transmission pathway. Where does modulation occur? - CORRECT ANSWERS 1. Cortex -> periaqueductal gray -> rostral ventral medulla -> dorsal horn
3. periaqueductal gray and rostral ventral medulla True or False: the descending pain transmission pathway modulates the emotional and sensory components of pain. - CORRECT ANSWERS False; just sensory. How do opioids affect potassium and calcium channels? - CORRECT ANSWERS 1. Potassium: opioids are agonists that bind to potassium channels and hyperpolarize the cell.
4. Calcium: opioids are agonists that bind to calcium channels and reduce opening and inhibit neurotransmitter release.

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The primary consequence of opioid overdose is _____________. - CORRECT ANSWERS respiratory depression Which effect from opioids has no tolerance? - CORRECT ANSWERS Miosis Which effect from opioids tends to be the worse dose limiting side effects? - CORRECT ANSWERS Constipation True or False: tolerance to opioids is a pharmacodynamic effect rather than pharmacokinetic. - CORRECT ANSWERS True Describe the mechanism associated with opioid tolerance. - CORRECT ANSWERS

1. Opioid receptors are phosphorylated and bound by arrestin.
2. Receptors are endocytosed. Name some symptoms associated with opioid withdrawal. - CORRECT ANSWERS
3. Early: Lacrimation, rhinorrhea, sweating.
4. 12-14 hours: dilated pupils, goosebumps, restlessness, tremor.
5. Peak: insomnia, abdominal cramps, exaggerated respiratory response, increased blood pressure, nausea. *Opposite of effects of opioids. True or False: short-acting opioids result in more intense, but shorter acting withdrawal symptoms. - CORRECT ANSWERS True

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Name 3 opioid agonsits that fall under the phenanthrenes class. - CORRECT ANSWERS 1. morphine

2. codeine
3. heroine True or False: morphine has low bioavailability and must be administered orally as codeine, IM or IV. - CORRECT ANSWERS True _______ and ______ are morphine pro-drugs. - CORRECT ANSWERS heroin and codeine Codeine is converted to morphine through ___________. - CORRECT ANSWERS demethylation Which enzyme is responsible for metabolizing codeine? - CORRECT ANSWERS CYP2D6 ____________ is a morphine-like semi-synthetic agonist that is orally active and potent as morphine. It may be used in combination with NSAIDs. - CORRECT ANSWERS Oxycodone ________________ is a morphine-like semi-synthetic agonist that is orally active but less potent than oxycodone. - CORRECT ANSWERS Hydrocodone

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What are the effects of dextromethorphan? - CORRECT ANSWERS Anti-tussive; no analgesic effects. ____________ is a very potent opioid agonist used in anesthesia to lower MAC of a general anesthetic. - CORRECT ANSWERS Fentanyl ____________ is an opioid agonist commonly used as an antidiarrheal. - CORRECT ANSWERS Loperamide ____________ is an opioid with similar analgesic efficacy as morphine, but it has a longer half-life. It is commonly used to treat opioid addiction. - CORRECT ANSWERS Methadone ___________ is a partial mu receptor opioid agonist with long duration of action used to treat opioid addiction. It has limited respiratory depression effects so it is considered a safer option. - CORRECT ANSWERS Buprenorphine _____________ is a partial kappa receptor opioid agonist used to treat chronic severe pain. - CORRECT ANSWERS Pentazocine ___________ is a pure opioid receptor antagonist with a short half life used to reverse opioid toxicity. - CORRECT ANSWERS Naloxone (narcan) True or False: narcan is typically administered orally. - CORRECT ANSWERS False; IV/nasal spray due to low bioavailability.