Previous chapters before the second midterm-----Q = 20 Flashcards

1
Q

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.

A

Pharmacokinetics

Pharmacodynamics:

Bioavailability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

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.

A

Passive

pH

lipid-soluble

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

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.

A

agonist

Efficacy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

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.

A

receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

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.
A

adrenal medulla

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Chapter 4 and 5: Cholinergic agonists & antagonists

Cholinergic RECEPTORS

2 types:
1. Muscarinic: M1 as ______ AND M2 as inhibitory receptors.

  1. Nicotinic: are located in CNS, adrenal medulla, ganglia, NM junctions. They show weak affinity for muscarine
A

excitatory

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Chapter 4 and 5: Cholinergic agonists & antagonists

Cholinergic AGONIST = (parasympathoMIMETIC):
EX.  Acetylcholine actions;
1. ↓ \_\_\_\_\_\_\_\_\_\_\_
 2. ↓ bl. Pressure
3. ↑ GI secretion & motility 
4. Causing miosis
A

heart rate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

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.

A

muscles paralysis.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

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 =_______________

A

hypotension

hypertension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

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

A

cardiac arrest

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

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 _______

A

Epinephrine

Norepinephrine

shock

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Chapter 6 / 7 Adrenergic agonist & antagonist

E. _____________ (synthetic β1 agonist)

  • —action: ↑ heart rate & ↑ cardiac output
  • — Uses: in congestive heart failure
A

Dobutamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Chapter 6 / 7 Adrenergic agonist & antagonist

  1. 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:

  1. orthostatic hypotension
  2. tachycardia
  3. vertigo
  4. sexual dysfunction
A

frostbite

hypertension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Chapter 6 / 7 Adrenergic agonist & antagonist

  1. 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
A

LOL = THEY ARE LAUGHING AT THE BETA’S BEING BLOCKED!

elderly & black

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Chapter 6 / 7 Adrenergic agonist & antagonist

Common side effects of β blockers:
=  HYPOtension,
= \_\_\_\_\_\_\_\_\_\_\_\_
=  fatigue
= drowsiness.
A

bradycardia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Chapter 6 / 7 Adrenergic agonist & antagonist

  1. 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

A

Guanethidine (Ismelin)

Cocaine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

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--- \_\_\_\_\_\_\_\_\_\_\_\_\_
A

Binding

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

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
A

acidic

pH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

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

A

peristalsis

cholinergic

anti- cholinergics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

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 ______ _______
A

2

4

activated charcoal

21
Q

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 _____________________

A

Protein

95

5

non-steroidal anti-inflammatory drugs (NSAIDs)

22
Q

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

A

Metabolism or biotransformation

cytochrome P450 (CYP)

23
Q

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

A

kidney

clearance

Diuretics

24
Q

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

A

safety

toxicities

age

25
Q

Anxiolytic & Hypnotic (chapter 9)

  1. BENZOdiazepines (e.g. Diazepam = Valium)

– Action: it binds to _____ receptors, to open Cl¯ channel →enhances __________ post-synaptic potential (IPSP).
1. ↓ anxiety
2. Sedation & hypnosis
3. Anticonvulsant
4. Muscle relaxant
—Uses: anxiety, seizure, muscle spasm or strain and sleep disorder (not in psychotic disorder).
– Side effects: drowsiness, confusion, psychological &
physical dependence, ↑ alcohol & CNS depression.

ZOlpidim (Ambien)

    • Acts on _____ receptors, uses in anxiety only.
  • – Side effects: nightmares, agitation, headache, drowsiness
A

GABA

inhibitory

GABA

26
Q

Anxiolytic & Hypnotic (chapter 9)

  1. Other anxiolytic & hypnotic drugs

SSRI group: Paroxetine (Paxil), Trazodone (desyrel),
Sertraline (Zoloft),& Fluoxetine (Prozac)

– Action: mediated by serotonin (5-HT1A) receptors, by
inhibit the re-uptake of ______ AND inhibit NE,M1receptors
—-Uses: only in anxiety
— Side effects: headaches, dizziness, nervousness

A

serotonin

27
Q

Anxiolytic & Hypnotic (chapter 9)

  1. BARBIturates (Phenobarbital)
    – Action:They were formerly used to sedate and induce sleep, by: binding GABA receptors and open the Cl¯ channels.
    – Uses: now mainly, as ___________ drug.
    – Side effect: drowsiness, impaired concentration, mental and physical sluggish, drug hangover, induce P-450 to
    ↓ other drugs duration of action.
  2. NON-barbiturate Sedatives
    A. _______ ________: it is a sedative and hypnotic
    (sleep between 1-6 hours).
    –Side effects: GI irritation, unpleasant taste sensation.
A

anticonvulsant

Chloral hydrate

28
Q

II. CNS Stimulants (chapter 10)

  1. Psychomotor Stimulants
    a. Methylxanthines
    b. Nicotine
    c. Cocaine
    d. Amphetamine
  2. Hallucinogens
    a. Lysergic acid diethylamide (LSD)
    b. Tetrahydrocannabinol (in marijuana)
    c. Phencyclidine (PCP)
A

KNOW

29
Q

II. CNS Stimulants (chapter 10)

Psychomotor Stimulants X 4

A. Methylxanthines

e. g. theophylline in tea, theobromine in cocoa, & caffeine in coffee, tea, cola drinks…
- – Actions: 1. stimulate the cerebral cortex → anxiety, tremors
2. +ve inotropic & chronotropic on the heart
3. Mild diuretic 4. ↑ gastric HCl secretion
- – Uses: in asthma (Theophylline)
- – side effects: insomnia, anxiety,

B. Nicotine

C. Cocaine
— Actions: blocks re-uptake of ________ from the ganglion to the neuron → causes stimulation of the
CNS, euphoria, feeling of well-being, hallucination, paranoia..
— Uses: ______ ____________ drug,
(causes vasoconstriction)
—side effects: - 1. Anxiety, as hypertension, tachycardia,

D. Amphetamine

    • Actions: similar to cocaine, due to ↑ NE in the synaptic space, → CNS stimulation, ↑alertness, insomnia, ↓ fatigue, ↓appetite.
    • Uses: limited
      1. Attention deficit syndrome (treated by methylphenidate = Ritalin HCl)
      2. ______________
A

norepinephrine

local anesthetic

Narcolepsy (sleep)

30
Q

Hallucinogens (chapter 10)

A. Lysergic acid diethylamide ———-(LSD)
— Action: It shows serotonin (5-HT) agonist at
pre-synaptic receptors in the midbrain.
——–Hallucination (__________)

B. Tetrahydrocannabinol (THC)

  • —– It contained in marijuana
  • –__________hallucinations, delusions
  • –Sometimes uses for _______ with cancer chemotherapy

C. Phencyclidine (PCP) = (angel dust)

  • –Actions: it inhibits the re-uptake of ___________, serotonin (5-HT) & norepinephrine (NE).
    1. hyper-salivation
    2. dissociative anesthesia
    3. It produces numbness of extremities, slurred speech
    4. It leads to hostile & bizarre behavior
A

color

Visual

vomiting

dopamine

31
Q

Antidepressant & Neuroleptic drugs–Chapters 12 & 13

—Feelings of sadness, hopelessness, despair, inability to experience pleasure in usual activities.
= (decreased ___ level)

—Enthusiasm, rapid thought and extreme self-confidence and impaired judgment. (⇧_____ level

A

NE

NE

32
Q

Antidepressant & Neuroleptic drugs–Chapters 12 & 13

  1. Tricyclic antidepressants (TCA): Imipramine, Desimipramine (Tofranil)
    — Actions: BLOCKS the NE & serotonin _____ into the neuron..TCA elevates mood, improves mental alertness,
    ↑ physical activity.
    —Uses: severe depression, some panic attacks, __________ for bed-wetting in children over 6 years old
A

re-uptake

imipramine

33
Q

Antidepressant & Neuroleptic drugs–Chapters 12 & 13

  1. Selective Serotonin-Reuptake inhibitors (SSRIs):Fluoxetine (Prozac)
    - - Actions: inhibit serotonin re-uptake, without anti-cholinergic, antihistamine nor α-blocker.
    - –Uses: _____ _______, bulimia , nervosa, obsessive-compulsive disorder, panic, PMS
  2. Monoamine Oxidase Inhibitors (MAO): (Phenelzine = Nardil)
    – Action: MAO inactivates the EXCESS neurotransmitter (NE), but the MAO inhibitors activate NE & serotonin
    receptors.
    — Uses: __________
    Side effects: Hypertensive Crises**
    —{Tyramine-induced hypertension}, if you use MAO
    inhibitors with certain foods contain tyramine (such
    as: old aged cheese, red wine, beer, chicken liver,
    pickled or smoked fish as anchovies),
A

major depression

depression,

34
Q

Neuroleptic drugs (Anti-psychotic drugs)–Chapter 13

To treat mainly schizophrenia.

— Schizophrenia is a type of psychosis, that is a mental
dysfunction. It is characterized by
1— delusion,
2—auditory hallucination,
3—and thinking or speech disturbance.
— Schizophrenia has a ______ component, due to some
biochemical abnormality,
(OVERACTIVE cerebral ____________ neurons)

A

genetic

dopaminergic

35
Q

Neuroleptic drugs (Anti-psychotic drugs)–Chapter 13

Neuroleptic drugs (Antipsychotic drugs)
– Action: block activity of ______AND ________ receptors in the brain.
- Uses:
1. Schizophrenia
2. Nausea & vomiting such as chlorpromazine AND
scopolamine.
3. Tranquilizer to treat agitation.

Side effects of neuroleptic drugs:
1.______________ effects= facial grimacing and
torticollis, static tremors,
2. ________ _________ (lateral jaw movements, AND “fly-catching” motions of the tongue).

A

dopamine and serotonin

Parkinsonian

Tardive dyskinesia

36
Q

Opioid analgesics

Opioid receptors: there are 4 families, in Greek
letters
1—–(µ = mu which is __________ receptors
2—-, κ =kappa, which is in the DORSAL horn
3——, σ =sigma, which is less specific,
4—— δ = delta, which is in the __________)

A

primary

periphery

37
Q

2 types of opioid analgesics:

I. Strong agonists:

A. MORphine

—-Actions: it affects _________ receptors, causes
hyperpolarization of the nerve cells, leads to:
analgesia (relief pain), euphoria (sense of well-being), REDUCE respiration, DEPRESS cough reflex, miosis(PΣ), vomiting, RELEASES histamine from mast cells.
—Uses: for PAIN, cough, & diarrhea (it ↓ motility).

Side effects of morphine:
1. Severe \_\_\_\_\_\_\_\_\_\_\_\_ depression.
2. Sedation (sleep)
3. Constipation, AND  vomiting.
4. Urinary retention, especially with prostatic hypertrophy,
5. It ↑ intracranial pressure (contraindicated
in head injury).
6. Addiction: tolerance AND  dependence
A

µ = mu

respiratory

38
Q

I. Strong agonists:

B. MEPeridine (Demorol)

— Actions: Meperidine binds to _______, opioid receptors,causes respiratory depression, cerebral vessels dilation, ↑_____ pressure, SMOOTH muscles contraction.
— Uses: in _____ ________ (analgesia).
— Side effects: tremor, hyperactive reflexes, hypotension.
Respiratory depression

A

κ = kappa

CSF

severe pain

39
Q

I. Strong agonists:

C. Methadone

–Actions: Methadone is a synthetic, mimic to
morphine, affects mainly µ = mu receptors.
– Methadone induces LESS euphoria but has a LONGER
duration of action
–Uses: to control the ________ ________ of heroin &
morphine addicts.

A

withdrawal effects

40
Q

I. Strong agonists:

D. Heroin

–Actions: it is synthetic from acetylation of morphine, which leads to ___-fold increase in its potency.
–It passes blood-brain barrier more rapidly than
morphine, which causes more euphoria.
–Uses: no medical use.

A

3

41
Q

II. Moderate agonists:

A. Codeine

Actions: Codeine is much less potent analgesic, less dependence, less euphoria than morphine. But, Codeine shows good antitussive activity.
Uses: in _________ __________ drugs,

A

cough prescription

42
Q

Drugs used to treat epilepsy

—Definition of epilepsy:
it is an abnormal electrical discharge of ________ neurons that cause seizures.
– Causes of epilepsy:
1. _______ epilepsy: idiopathic, may be due to an inherited
abnormality in the CNS.
2. _______ epilepsy: as tumors, head injury, hypoglycemia, meninigitis…

A

cerebral

Primary

Secondary

43
Q

Drugs used to treat epilepsy

Types of epilepsy

  1. Partial (focal):
    a. SIMPLE: a single limb or a muscle
    b. COMPLEX: different disorders
  2. Generalized:
    a. tonic-clonic (_____ _____): most dramatic form, aura
    b. absence (____ _______): young child
    c. MYOclonic: muscle contraction WITHOUT seizure
    d. FEBRILE seizure: associate with high fever in children
    e. status epilepticus: _________ recurrent
A

grand mal

petit mal

rapidly

44
Q

Drugs used to treat epilepsy

Anticonvulsant agents

  1. Phenytoin (Dilantin)

—Actions: decreases the influx of ___AND___ in neurons during depolarization.
— Uses: for all partial seizures, tonic-clonic seizure AND status epilepticus.
SE—______ __________ (the gums grow over teeth) in
children.

A

Na+ and Ca++

gingival hyperplasia

45
Q

Drugs used to treat epilepsy

Anticonvulsant agents

  1. Carbamazepine (Tegretol)
  • Actions: it blocks the ____ channels to INHIBIT impulses in the brain.
    • Uses: FIRST CHOICE drug in all partial seizures. And also, for tonic-clonic seizures.
    • Side effects: it causes: stupor, coma, respiratory depression, with drowsiness, vertigo, ataxia & blurred vision
A

Na+

46
Q

Drugs used to treat epilepsy

Anticonvulsant agents

  1. Phenobarbital (Bellatal oral or Luminal injection)
  • —Actions: Phenobarbital as antiepileptic drug through ______ neurons.
  • —Uses: in simple partial seizures, febrile seizures (as well as Valium) and recurrent tonic-clonic seizures.
  • —Side effects: sedation
  1. EthoSUXimide (Zarontin)
    – Actions: it reduces propagation of abnormal electrical
    activity in the brain.
    – Uses: it is the first choice in ______ ______ epilepsy
    – Side effects: nausea,
A

GABA

absence (petit mal)

47
Q

Insulin

3 types:

  1. Short acting (regular):lispro PEAK in 20 minutes and regular in 2 hours
  2. Intermediate neutral protamine hagedorn (NPH): PEAK in ___ hours
  3. Long acting (glargine, detemir): NO PEAK but it stays __ hours
  • -Side effects of insulin is _____________
  • -Caution to use these drugs with liver, heart or kidney dysfunction
A

6

24

hypoglycemia:

48
Q

Oral agents

1—primary is tolbutamide (orinase) for 6-12 hrs
2—-and second generation is glipizide (glucotrol) for 24 hrs

Action:

  1. stimulate insulin release from the ________
  2. Reduce_______ glucose production
  3. Increase _____________insulin sensitivity
A

pancreas

liver

peripheral