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Topic 3
Ototoxicity
34
Audiology
Graduate
09/06/2017

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Term
a drug’s ability to produce ototoxic effects involves ___ and ___.
Definition
pharmacodynamics and pharmacokinetics
Term
Pharmacodynamics:
-Related to drug's mechanism of ___
-___ and ___ drug-receptor interaction
-Process: Drugs go to ___. The target is usually the ___ ___ surface. Then it begins a ___-___ process.
Definition
action; Lock and key; target; cell membrane; multi-step
Term
What are a few examples of receptors that lead to processes?
Definition
-transmembrane ion channels
-transmembrane receptors linked to intracellular g proteins
-transmembrane receptors linked to cystolic enzymes
Term
Lock and Key Model: what are the keys and what are the receptors?
Definition
Keys=drugs, neurotransmitter, and ligands. Locks=receptors
Term
___ is a molecule, as an antibody, hormone, or drug, that binds to a receptor
Definition
Ligand
Term
What are some neurotransmitters?
Definition
Acetylcholine (Ach), dopamine (DA), and epinephrine
Term
Drugs that can block or reduce action of agonists (or neurotransmitters) by direct or indirect ways.
Definition
Antagonists
Term
Examples of Antagonists:
-___ ___: block the effect of NE; affects blood pressure & heart rate by blocking the effect of NE (natural agonist)
-___ and ___ (Ach receptor antagonists) to treat vertigo & Meniere’s disease
-“____” dephenlhydramine (Benedryl) is a histamine receptor antagonist
Definition
Beta blockers; Scopolamine and meclizine; antihistamine
Term
Antagonist can also target enzymes. What is an example?
Definition
Ibuprofen: a non-steroidal, anti-inflammatory drug (NSAID) which inhibits the enzyme cyclooxygenase to help form inflammatory prostaglandins
Term
How is the effectiveness of a drug described?
Definition
Using a dose-response curve
Term
Dose-Response Curves...
-describes a drug's ability to cause a ___
-shows relationship of a given dose to the ___ ___ (desired effect or unwanted toxic effect)
Definition
response; measured response
Term
drug’s ability to elicit maximum response at a given dose; drug’s ability to treat a disease
Definition
Efficacy
Term
Amount of a drug needed to produce 50% of a drug’s potential max response
Definition
Potency
Term
Therapeutic Index:
-Ratio of a drug’s ___ dose to its therapeutic dose (or plasma
concentration)
-Small ratio between toxic dose and therapeutic dose =___ therapeutic index
-Large ratio between toxic dose and therapeutic dose =___ therapeutic index
Definition
toxic; small; large
Term
Small Therapeutic Index:
-small ratio between ___ and ___ effects
-narrow window between ___ and ___
-dangerous effects are common at ___ doses.
Definition
unwanted & wanted; efficacy; toxicity; normal
Term
Large Therapeutic Index:
- ___ ratio between wanted and unwanted effects
- ___ window between efficacy and toxicity
-dangerous effects _____ at normal doses
Definition
large; wide; not common
Term
___ is he expression of a genetic code
Definition
Polymorphism
Term
Dose-Response versus Dose-Toxicity:
-shows dose of drug X needed for a ___ response
-Increasing dose can ___ efficacy
-as dose increases, risk of ___ effects increases too
-at a certain point, some meds reach ___ benefit, & further dose increases only increase risk of ___ effects
Definition
therapeutic; increase; toxic; maximum; adverse
Term
What does pharmacokinetics consist of?
Definition
Absorption, distribution, metabolism, and excretion and elimination
Term
Absorption depends on routes of ___
Definition
administration
Term
Amount of Absorption may depend on…
-stomach ___
-drug’s physical and ___ characteristics
-consumption of other ___ or ___
-dosage ___ (slow-release)
-bioavailability: actual ___ of the drug that reaches the systemic circulation
-extent of first-pass metabolism by the ___
Definition
PH; chemical; drugs; food; formulation; amount; liver
Term
___ is the drug’s movement to target site(s) of action
Definition
distribution
Term
are protective mechanisms within the body
Definition
barriers
Term
What are some barriers in the body?
Definition
blood-brain barrier, blood-testes barrier, and blood-placental barrier
Term
-as drug starts circulating, liver starts to ___ it
-enzymes are broken down to make molecules more ___ soluble (and able to be excreted by kidneys).
Definition
metabolize; water
Term
Phase I Metabolism-modify drug structure through:
-____: is the chemical breakdown of a compound due to its reaction with water
-___: is a chemical reaction that moves electrons
-___: is elimination of a compound
Definition
hydrolysis; oxidation; reduction
Term
Phase II Metabolism:
-involve conjugative reactions that act to combine drugs with large, water soluble ___ molecules to enhance a drug’s solubility and excretion into urine
Definition
polar
Term
What is the main route of excretion and elimination of drugs?
Definition
The kidneys
Term
Excretion & Elimination:
-renal function gets worse with increasing ___
-___ excretion is the secondary route
-doses are often adjusted for those with ___ renal function
Definition
age; biliary; compromised
Term
Kidneys:
-regulate ___ composition
-keep volume of ___ constant
-remove ___ (urea, ammonia, drugs, toxic substances)
-maintain the ____ concentration of blood
-help regulate blood ___
-stimulate production of ____
-maintain body's ___ levels
Definition
blood; water; wastes; acid/base; pressure; RBCs; calcium
Term
-peak concentration in plasma shows ___ distribution
-therapeutic activity- occurs above a certain ___ concentration (while staying below toxic levels)
-elimination- the drug becomes ___ active (levels are below
minimally effective plasma concentrations)
Definition
maximum; minimal; less
Term
___ is the time it takes for a drug’s plasma concentration to decrease by 50%
Definition
Half-life
Term
Half-Life:
-___ for individuals
-affected by ___-___ interactions, drug-food interactions, ___ changes, or impaired kidney function
Definition
varies; drug-drug; metabolic
Term
How Plasma Concentrations Change Over Time:
-___ ___: point when the amt of drug given equals the amt of drug eliminated in one half-life
-___ ___: time it takes for a drug to no longer be detected in plasma
Definition
steady state; washout period
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