ANSTH - PHRMA Flashcards by 18 22

Time dependency of the drug

a. Pharmacokinetics
b. pharmacodyanmics
c. Potency
d. Efficacy

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True about pharmacokinetics EXCEPT

a. time dependency of the drug
b. describes the relationship between the dose of a drug and its plasma or tissue concentration
c. relates to absorption, distribution, metabolism and elimination
d. What the drug does to the body

it is the definition of pharmacodynamics

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How the plasma concentration of a drug translates into its effect on the body. This is called

Pharmacodynamics

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True about Pharmacokinetics

a. oral, IV and nasal or sublingual route are subject to first pass effect
b. Moecular size of drug, capillary permability, polarity and lipid solubility affec rate of entry of drug into tissues
c. Theoretical volume that would be necessary to contain the total amount of an administered drug at the same concentration that it is observed in the blood plasma is called volume of distribution
d. AOTA

A. nasal or sublingual bypass first pass effect

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Drugs that interact with and activate receptors; they possess both affinity and efficacy. Full efficacy

Full agonist

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Pharmacologic antagonist that competes with agonist for receptor binding site

Competitive inhibitor

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Drugs that interact with receptors in such a way that they have affinity but NO efficacy

Competitive inhibitor

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Act different sites of receptor molecules (does not compete), and activates it. Alter receptor function without occupying it.

Allosteric activator

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Reverse effect and action of allosteric activator

Allosteric inhibitor

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Mechanisms of Desensitization

Downregulation

Upregulation

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short-term diminution of receptor response caused by frequent or continuous exposure to agonists

Tachyphylaxis

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Which drug would be absorbed first?

a. Gas
b. Solid
c. Liquid

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What is the bioavailability of an IV drug?

100%

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This is the apparent volume of fluid into which the drug appears to distribute itself at a concentration equal to that in the plasma.

Volume of distribution

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True about volume of distribution

a. high volume of distribution means it is concentrated in the vascular space
b. minimal volume of distribution means that the drug is mostly in the extravascular space
c. both
d. neither

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Defined as the percentage of the active drug in a drug product that enters the systemic circulation as a parent compound after the administration of that drug

Bioavailability

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The rate of elimination by all routes normalied to the drug

concentration

Drug clearance

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dose required to produce a given effect

Potency

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Power to produce effect

Efficacy

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Dose producing the desired effect in 50% of the general population

ED50

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shiw relationship between the dose of the drug admnistered and the pharmacologic effect of the drug

Dose response curves

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dose producing death in 50% of animals to which it is given

LD50

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LD50/ED50

therapeutic dose

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Dose that brings toxicity in 50% of humans

TD50

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Types of anesthesi (3)

Local Regional Spinal

Triad of 3 major effects in anesthesia

UAM Unconsciousness Analgesia Muscle relaxation

IV agents that provude unconsciousness and amnesia EXCEPT a. barbiturates b. propofol c. benzodiazepines d. etomidate e. succinylcholine

E; muscle relaxant

Which drug is this? MOA: inhibit excitatory synaptic transmission at the GABA receptor Effect: rapid & smooth induction within 60 secs- wears off in 5 mins S/E: hypotension, myocardial depression Adv: anticonvulsants, protect brain during neurosurgery by cerebral metabolism

Barbiturates

Which drug is this? MOA: inhibit excitatory synaptic transmission at the GABA receptor Effects: anxiolysis, amnesia (anterograde) S/E: peripheral vasodilation, hypotension, minimal resp depression when used alone Adv: anticonvulsant, rarely cause allergic reactions Flumazenil- reverses BZD effects; antagonist

Benzodiazepines

Which drug is this? MOA: inhibit excitatory synaptic transmission at the GABA receptor Effects: rapid induction Adv: less reduction in blood pressure than thiopental & propofol, rapid awakening Disadv: pain on injection, nausea & vomiting

Etomidate

Which drug is this? MOA: inhibits excitatory synaptic transmission at the GABA receptor Effects: fast onset of sedation, short duration, rapid recovery (choice for ambulatory surgery) Adv: low incidence of nausea and vomiting, bronchodilatory properties S/E: hypotension, irritant pain on injection

Propofol

Which drug is this? MOA: inhibit excitatory synaptic transmission at the NMDA receptor Effects: amnesia and analgesia S/E: dissociative anesthetic, cataleptic state and hallucinations while regaining consciousness Disadv: increase HR & BP (CI: CAD pxs); direct myocardial depression in catecholamine depleted pxs Adv: useful in acutely hypovolemic pxs to maintain BP via sympathetic stim; asthmatic pxs- bronchodilation, less allergic reactions

Ketamine

The following are used to provide analgesia EXCEPT a. ketamine b. morphine c. propofol d. ketorolac

C. propofol is for unconsciousness and amnesia. Ketamine is both for unconsciousness and amnesia, and analgesia

pure opioid antagonist; reverse opioid overdose (resp depression)

Naloxone/naltrexone

Which drug is this? MOA: act centrally on μ-receptors on the brain & SC S/E: euphoria, sedation, constipation, resp depression

Opioid

MOA: inhibit excitatory synaptic transmission at the NMDA receptor Effects: potent analgesic, sedation & amnesia Adv: supports respiration Disadv: dysphoria

Ketamine

Which drug is this? MOA: reduces prostglandin formation via inhibition of the COX enzyme (NSAID) S/E: gastric bleeding, platelet dysfunction, hepatic and renal damage

Ketorolac

``` Which drug is this? MOA: a2 adrenergic agonist Effects: sedative & analgesic Uses: sedation in ICU, adjunct to GA S/E: hypotension and bradycardia ```

Dexmedetomidine

Which drug is this? MOA: centrally acting Effects: analgesic & antipyretic When used as part of post-op analgesic property, it reduces amount of opioid required  reduced opioid S/E (constipation, sedation, resp depression)

Acetaminophen

True about neuromuscular blocking agents EXCEPT a. No amnestic, hypnotic or analgesic properties b. this is given prior to analgesia c. act on neuromuscular junction d. succinylcholine is a depolarizing NMB e. NOTA

B. pxs must be properly anesthetized first before its administration

Which drug is this? Depolarizing NMB MOA: binds to Ach receptors on the postjunctional membrane in the NMJ and causes depolarization of muscle fibers Adv: Rapid onset (<60 secs) & rapid offset (5-8 mins) DisAdv: Fasciculations causes post-op aches and pains; elevates serum K levels (CI in burns & trauma pxscardiac arrhytmias); increase in intraocular and intragastric pressure Hydrolyzed by plasma cholinesterase or pseudocholinesterase Can trigger malignant hyperthermia

Succinylcholine

Examples of Non-depolarizing NMB (4)

Pancuronium Vecuronium Rocuronium Mivacurium

Non-depolarizing NMB with >1h duration of effect, no histamine release, disadvantage of Tachycardia;Slow onset; Long duration.

Pancuronium

Non-depolarizing NMB with <1 h effect, No CV effects, disadvantage of intermediate onset

Vecuronium

Non-depolarizing NMB with <1h effect, fast onset, short duration and histamine release

Mivacurium

Non-depolarizing NMB, <1h effect, fast onset, No CV effects

Rocuronium

True about non-depolarizing NMB EXCEPT a. irreversibly binds to post synaptic terminal in the NMJ and prevents Ach from depolarizing the muscle b. No fasciculations c. both d. neither

A. it is reversible

This is a Measure of anesthetic potency. It is the ED50 of an inhaled agent The higher the the value, the less potent the agent is

MAC (Minimum alveolar concentration)

Most potent inhalational agent among the list: a. halothane b. NO c. Enflurane d. Desflurane e. Sevoflurane

Which drug is this? MAC 105%, provides analgesia with minimal cardiac and respiratory depression. Disadvantage of sympathetic stimulation, expansion of closed airspace.

Which inhilational agent is this? MAC of 0.75, effective in low concentration, minimal airway irritability, inexpensive. Disadvantage of cardiac depression and arrhythmia; hepatic necrosis; slow elimination

Halothane

Which inhalational agent is this? MAC is 1.68, Muscle relaxation, no effect on cardiac rate and rhythm; disadvantage of strong smell and seizures

Enflurane

Which inhalational agent is this? MAC 6 rapid induction and emergence, disadvantage is coughing and high cost

Desflurane

Which inhalational drug is this? MAC is 1.15, advantage is muscle relaxation, no effect on cardiac rate and rhythm. Disadvantage is strong smell

Isoflurane

Which inhalational drug? 1.71 MAC, rapid induction and emergence, pleasant smell; ideal for mask induction; disadvantage is high cost and liver metabolism

Sevoflurane

True about local anesthetics EXCEPT a. amide local anesthetics have amide linkage between a benzene ring and a hydrocarbon chain that in turn, is attached to a tertiary amine b. Lidocaine, bupivacaine and procaine are examples c. Metabolized in the liver d. NOTA e. AOTA

B. procaine is an ester. ``` Lidocaine Bupivacaine Mepivacaine Prilocaine Ropivacaine ```

True about local anesthetics a. Cocaine, procain, cchlorprocaine, tetracaine, benzocaine, and prilocaine are esters b. esters are hydrolysed by plasma cholinesterase c. esters have allergic potential d. AOTA e. NOTA

A. Prilocaine is an amide

The ff are metabolized in plasma EXCEPT a. procaine b. Chloroprocaine c. Prilocaine d. Tetracaine e. NOTA

C; amides are metabolized in the liver. All the other 3 are esters and are metabolized in plasma.

The ff are metabolized in the liver and lung a. Prilocaine b. lidocaine c. mepivacaine d. bupivacaine e. Ropivacaine

Only prilocaine is metabolized in the liver and lung A.

What is the MOA of local anesthetics

Reversible block of the transmission of neural impulses when placed on or near a nerve membrane by stabilizing sodium channels in theirclosed state, preventing action potentials from propagating along the nerve

True about local anesthetic toxicity EXCEPT a. CNS toxicity occurs earlier than Cardiovascular system toxicity b. Restlessness -> slurred speech-> tinnitus-> seizures-> unconsciousness c. mgt of CNS toxicity is benzidiazepine/thiopental for seizures, and airway mgt d. NOTA

B ``` restlessness tinnitus slurred speech seizures unconsciousness ```

True about Cardiovascular system toxicity in local anesthetic a. hypotension-> increased P-R intervals -> bradycardia-> cardiac arrest b. Bupivacaine is very cardiotoxic c. Lidocaine toxic dose is 5 mg/kg d. NOTA e. AOTA

Calculate the volume of 0.5% bupivacaine needed to administer 3mg/kg to a 50kg person.

30mL