Previous chapters before the second midterm-----Q = 20 Flashcards
Chapter 2: Pharmacokinetic & drug receptors
_______________: the action of the body on the drugs
(absorption, distribution, metabolism & elimination).
_____________ the action of a drug on the body.
__________–amount of drug reaches the blood without
changes.
Pharmacokinetics
Pharmacodynamics:
Bioavailability
Chapter 2: Pharmacokinetic & drug receptors
Absorption of drugs:
A. Transport of drugs from the GI tract:
1. ___________ diffusion
2. Active transport & cotransport (Na+)
B. effect of _____ (weak acid or weak base) on drug absorption
Bio-transformation of the drug, mostly in the LIVER, especially the ______________ drugs.
Passive
pH
lipid-soluble
Chapter 2: Pharmacokinetic & drug receptors
An _______: is an agent that can bind to a receptor & elicit a response.
________: is the maximal response produced by
the drug.
agonist
Efficacy
Chapter 3: The Autonomic Nervous System
Σ preganglionic fibers arise from thoracic & lumber regions, ganglions are located close to the spinal cord
PΣ preganglionic fibers arise from cranial and sacral areas, and ganglions are located close to the effector organs.
Neurotransmitters are:
a. acetylcholine
b. norepinephrine
________: is a recognition site for a binding chemicals and processes a response.
receptor
Chapter 4 and 5: Cholinergic agonists & antagonists
The cholinergic NEURONS include: 1--- \_\_\_\_\_\_\_\_ \_\_\_\_\_\_\_\_\_\_ (preganglionic), 2---autonomic ganglia (Σ & PΣ) 3---postganglionic fibers of PΣ 4---- neuromuscular (NM) junction.
adrenal medulla
Chapter 4 and 5: Cholinergic agonists & antagonists
Cholinergic RECEPTORS
2 types:
1. Muscarinic: M1 as ______ AND M2 as inhibitory receptors.
- Nicotinic: are located in CNS, adrenal medulla, ganglia, NM junctions. They show weak affinity for muscarine
excitatory
Chapter 4 and 5: Cholinergic agonists & antagonists
Cholinergic AGONIST = (parasympathoMIMETIC): EX. Acetylcholine actions; 1. ↓ \_\_\_\_\_\_\_\_\_\_\_ 2. ↓ bl. Pressure 3. ↑ GI secretion & motility 4. Causing miosis
heart rate
Cholinergic ANTAGONIST (parasympathoLYTIC)
• 3 types: • 1. Muscarinic receptor BLOCKER: e.g. atropine---1. Atropine • Action: blocks the central & peripheral muscarinic receptors, (by competitive antagonist) AND scopalamine--for motion sickness
• 2. Ganglion BLOCKER:
e.g. nicotine
• 3. Neuromuscular BLOCKER:
e.g. tubocurarine— may cause histamine release & __________ ___________ Uses: during surgery, to relax skeletal muscle.
EX. succinylcholine—during the induction of
anesthesia, & during electroconvulsive (EC) shock treatment.
muscles paralysis.
Chapter 6 / 7 Adrenergic agonist & antagonist
Action of the α- adrenoreceptors
α-1
1. Smooth ms contraction
USE THIS WHEN YOU HAVE=_________, local anesthesia
α-2
1. Smooth ms relaxation
USE THIS WHEN YOU HAVE =_______________
hypotension
hypertension
Chapter 6 / 7 Adrenergic agonist & antagonist
Action of the β- adrenoreceptors
β-1
1.↑ heart rate (tachycardia)
USE THIS WHEN YOU NEEDTO FIX A
__________ ______________
β-2
1.vasodilation of the BV
USED FOR bronchospasm
cardiac arrest
Chapter 6 / 7 Adrenergic agonist & antagonist
Adrenergic agonist = sympathoMIMETIC
A. ____________ (Adrenaline): = ↑heart rate
Side effects: anxiety, tension, headache,
tremor, cerebral hemorrhage, arrhythmia
B. _____________
Action: It is less potent than epinephrine, affects α-
adrenergic receptors.
—It causes: vasoconstriction, ↑cardiac contraction
(=inotropic)
— Uses: treat shock, however, dopamine is better.
C. Isoproterenol, (synthetic adrenergic agonist)
D. Dopamine–Uses: dopamine is the drug of choice for _______
Epinephrine
Norepinephrine
shock
Chapter 6 / 7 Adrenergic agonist & antagonist
E. _____________ (synthetic β1 agonist)
- —action: ↑ heart rate & ↑ cardiac output
- — Uses: in congestive heart failure
Dobutamine
Chapter 6 / 7 Adrenergic agonist & antagonist
- α-blockers–Alpha blockers cause blood vessels to dilate, thereby lowering blood pressure
A. PHENTOlamine (Regitine) = to treat ______
B. PRAZOsin (Minipress)–to decrease ________
Side effects of α-blockers:
- orthostatic hypotension
- tachycardia
- vertigo
- sexual dysfunction
frostbite
hypertension
Chapter 6 / 7 Adrenergic agonist & antagonist
- β-blockers–Beta-blockers are medicines used to treat high blood pressure, congestive heart failure, abnormal heart rhythms, and chest pain.
A- PropranoLOL (inderal)--USED FOR Uses: 1. HYPERtension 2. Migraine Side effects: = bronchoconstriction B- AtenoLOL (tenormin) ---Action: selective β1 blocker, ↓ BP --- Uses: in HYPERtension C. LabetoLOL (Normadyne) ---- Action: β1& β2 blocker and α1 antagonist, produces peripheral vasodilation & ↓ BP ---Uses: \_\_\_\_\_AND \_\_\_\_\_\_\_ hypertensive patients
LOL = THEY ARE LAUGHING AT THE BETA’S BEING BLOCKED!
elderly & black
Chapter 6 / 7 Adrenergic agonist & antagonist
Common side effects of β blockers: = HYPOtension, = \_\_\_\_\_\_\_\_\_\_\_\_ = fatigue = drowsiness.
bradycardia
Chapter 6 / 7 Adrenergic agonist & antagonist
- Drugs affecting neurotransmitter release or uptake
1–___________________
—-Action: it BLOCKS the RELEASE of NE → ↓ BP.
Uses: in hypertension
Side effect: orthostatic hypotension
2—__________
— Action: it BLOCKS the UPTAKE of the neurotransmitter (NE) by the adrenergic neuron, → accumulation of NE in the
synaptic space → ↑ sympathetic activity → CNS
stimulants & drug of abuse
Guanethidine (Ismelin)
Cocaine
Drug-Herb Interactions—Chapter 3
There are three main areas of concern with absorption in regard to drug-herb interactions: 1--- Acidity 2---Gastrointestinal motility 3--- \_\_\_\_\_\_\_\_\_\_\_\_\_
Binding
Drug-Herb Interactions—Chapter 3
Acidity
- —Acidity, or pH, plays a large role in absorption for some agents
- – Some drugs need a very _______environment in order to be absorbed, often in order to convert a drug into a form that is easily absorbable
- —_____ can also affect whether an agent is charged or neutral which has direct consequences as to whether it can easily pass through cell membranes
acidic
pH
Drug-Herb Interactions—Chapter 3
Gastrointestinal Motility
– GI motility mainly refers to intestinal __________
– Increased peristalsis means a FASTER intestinal transit
time, LESS contact with the wall of the intestines and
therefore LESS ability for absorption of the substance
– Of course, the opposite is also true.
– Either of these can have helpful or detrimental effects
– INCREASED motility of the GI tract may happen when
using _________ agents and prokinetic
gastrointestinal agents such as metoclopramide and
cisapride
— DECREASED peristalsis may occur when using
____-_______, narcotics, phenobarbital, and to a lesser
extent some anti-depressants and antipsychotics
peristalsis
cholinergic
anti- cholinergics
Drug-Herb Interactions—Chapter 3
Binding
- —There are some drugs and herbs that are cloying and sticky and can adhere to other substances consumed at the same time
- -While often this is due to the inherent nature of the drug or herb, sometimes it is the function of the drug as in the case of cholestyramine which is designed to sequester bile and cholesterol within the intestines and NOT allow them to be (re)absorbed
- – In general, anything taken between __ hours before or ___ hours after these substances will NOT be absorbed well
- – Drugs that are binding include the bile acid sequestrants, sucralfate, and ______ _______
2
4
activated charcoal
Drug-Herb Interactions—Chapter 3
Distribution
– ____________ binding is by far the biggest factor when determining interactions
– Drugs or herbs with active ingredients that are HIGHLY
protein bound are very susceptible to interactions
– Highly protein bound substances are over ___% bound
– That means less than ___% of the agent is actually FREE and able to EXERT its EFFECTS
– Therefore even a very small displacement of the bound
substance could result in a dramatic increase in the
amount of free agent and hence a huge difference in the
agent’s effects
—Drugs that are highly protein bound and therefore
open to these types of interactions include warfarin,
phenytoin, oral contraceptive pills, and _____________________
Protein
95
5
non-steroidal anti-inflammatory drugs (NSAIDs)
Drug-Herb Interactions—Chapter 3
_________OR___________ of substances,
has a large potential for interactions
— There are many factors that affect metabolism
including genetics, gender, the organ health of the
liver and kidneys, organ maturity, blood pressure,
diet, and whether the patient is a smoker or regular drinker of alcohol
—One of the biggest targets of interactions within
the realm of METABOLISM is the _____________ system
**ALCOHOL CAN INDUCE OR INHIBIT THIS
**GRAPEFRUIT CAN INHIBIT TOO
Metabolism or biotransformation
cytochrome P450 (CYP)
Drug-Herb Interactions—Chapter 3
Elimination
– Elimination which can occur through many routes, but
primarily the ______, can be affected by the health of the
kidneys, organ maturity, volume of distribution, perfusion of the kidneys, and urinary pH
– The most significant factor in determining interactions is
how a substance affects _____________
– Patients on dialysis or who have had a kidney transplant may have significantly impaired elimination from the kidneys
–_______ can increase clearance from the kidneys
— Theoretically, herbs in the drain damp category may
hasten renal clearance
kidney
clearance
Diuretics
Drug-Herb Interactions—Chapter 3
Therapeutic Margin
—Since the therapeutic margin is a direct measure of the _______ of a drug, any substance that has a NARROW margin may have significant ________ if thrown out of
that range
—- What may or may not push an agent out of the safety margin is an individual response and may be predicated on many factors such as the ____ and gender of the patient, dietary changes, and what OTHER DRUGS the patient may be taking
safety
toxicities
age
