Questions 1-16 p1 Flashcards

1
Q

What is pharmacokinetics?

A

The study of the process of drugs in the body.

ADME

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2
Q

What are the 4 processes involved in pharmacokinetics?

A

ADME

  1. Absorption
  2. Distribution
  3. Metabolization
  4. Excretion
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3
Q

What 2 things determine the rate of absorption?

A
  1. Lipid Solubility

2. Drug Ionization

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4
Q

What form must drugs be in to be absorbed?

A

unionized

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5
Q

What form must drugs be in to be excreted?

A

ionized

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6
Q

What are the 3 main factors that influence distribution?

A
  1. Plasma Protein Binding
  2. Blood Flow
  3. Blood Brain Barrier
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7
Q

What 3 organs get the majority of distribution and why?

A

Blood Flow is the reason

  1. Kidney
  2. Liver
  3. Brain
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8
Q

What is another name for metabolism?

A

Biotransformation

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9
Q

What organ mainly handles metabolism?

A

Liver

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10
Q

What is the system in the liver that handles metabolism?

A

DMMS

Drug Microsomal Metabolizing System

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11
Q

What is the enzyme in the DMMS system and what does it do?

A

Cytochrome P450

Turns lipid soluble drugs into water soluble drugs for excretion

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12
Q

If a drug is significantly metabolized initially what do we call this and what can you do to overcome this phenemenon?

A

First Pass

Loading Dose

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13
Q

Lastly, what organ handles excretion?

A

Kidney

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14
Q

What form must a drug be into be excreted?

A

Ionized

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15
Q

What 2 factors affect excretion?

A
  1. acidic urine

2. Renal Blood Flow

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16
Q

What is LD50 and what is it used for?

A

Lethal Dose for 50% of test animals

Done to determine the lethal/toxic dose

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17
Q

What is ED50 and what is it used for?

A

Effective Dose for 50% of human population

Done to determine the dose at which 50% of population will experience therapeutic benefit

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18
Q

What is TI and what is it used for?

A

Therapeutic Index
Calculation: TI = LD50/ED50
Done to determine the relative safety of the drug

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19
Q

What is the GOAL of drug therapy?

A

To achieve therapeutic effect with little to no adverse or toxic effects

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20
Q

What is the SODAS system and what does it achieve?

A

Spherical Oral Drug Absorption System

Different Layers that dissolve in different time frames for delayed dosing (1 pill - longer effect)

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21
Q

What is the GITS system and what does it achieve?

A

Gastrointestinal Therapeutic System
Bi-layer pill with tiny hole and internal membrane that allows for immediate dosing with a time delay for a second dose (1 pill - longer effect)

22
Q

What are the factors that determine how much drug reaches a particular organ?

A
  1. Plasma Protein Binding
  2. Blood Flow
  3. Blood Brain Barrier
23
Q

What are the 4 factors of bioavailability (directly releated to plasma protein binding)?

A
  1. Bioavailability (drug formulation)
  2. Route of Administration
  3. Factors that effect GI absorption
  4. Individual Variation
24
Q

What are the individual variation factors?

A
  1. Age
  2. Weight
  3. Gender
  4. Genetics
  5. Emotional State
  6. Placebo
  7. Presence of Disease
  8. Patient Compliance biggest downfall
25
Q

What can decrease effectiveness of DMMS?

A

too many drugs, so all enzymes are used up

26
Q

What is enzyme induction?

A

Where the liver produces more enzyme to deal with that drug and hence the drug is metabolized faster and so the same dose no longer produces the same therapeutic effect

27
Q

Why is the lipid solubility of a drug so important?

A
For absorption reasons
1. must be water soluble to be transported
2. must be lipidy enough to enter cells
most drugs are BOTH
BUT must be super lipidy to cross BBB
28
Q

Which nerves extending from the spinal cord regulate the parasympathetic nervous system?

A

Cranial and Sacral Nerves

29
Q

Which nerves extending from the spinal cord regulate the sympathetic nervous sytem?

A

Thoracic and Lumbar Nerves

30
Q

What is Monoamine oxidase and what does it do?

A
An enzyme (a protein) that breaks down 
NE and EPI and Serotonin
31
Q

Where are alpha receptors found?

A
Alpha 1 = 
1. blood vessels
2. iris
3. gastro and urinary sphincters
Alpha 2 = 
found in adrenergic nerve endings
32
Q

What happens when NE/EPI bind with alpha 1 receptors?

A
  1. Stimulates vasoconstriction of blood vessels
  2. stimulates constriction of iris = mydriasis (pupil dilation)
  3. stimulates contraction of GI and Urinary sphincters decreasing movement
33
Q

What happens when NE/EPI stimulate alpha 2?

A

typically inhibit further release of NE

34
Q

What are the CLINICAL INDICATIONS for use of alpha adrenergics?

A
  1. Hypotension (low bp)
  2. Need Mydriasis (pupil dilation)
  3. Congestion (vasoconstriction)
35
Q

Which receptors do EPI stimulate?

A

alpha 1 and 2

beta 1 and 2

36
Q

What are the SE of beta blockers?

A

SE =

  1. N/V/D
  2. Dizziness
  3. Drowsiness
  4. Depression
37
Q

What are the AE of beta blockers?

A

AE =

  1. Hypotension
  2. Bradycardia
  3. Bronchostriction
38
Q

Which receptors do SELECTIVE beta adrenergic blocking drugs affect?

A

Beta 1 Blockers (smooth and cardiac muscle - mainly heart)

39
Q

Where do you find Beta 2 receptors?

A

Smooth and Cardiac muscle - but mainly LUNGS

40
Q

A patient has asthma and hypertension, which beta blocker should you use?

A

Selective Beta 1 Blocker
Atenolol/Tenormin
Metoprolol/Lopressor

41
Q

List the types of cholinergic receptors, what they bind with and where they are found.

A
  1. Cholinergic/Muscarinic, ACH, Parasympathetic Nervous System (post ganglionic nerve endings)
  2. Cholinergic/Nicotinic I, ACH, Parasympathetic AND Sympathetic ganglionic nerve endings
  3. Cholinergic/Nicotinic II, ACH, Somatic Nervous System (skeletal muscle, Voluntary)
42
Q

Where are nicotinic I receptors located and in what nervous system?

A

Nicotinic I (cholinergic)
ANS - Parasympathetic AND Sympathetic
Ganglionic Nerved Endings

43
Q

What is the MOA for centrally acting skeletal muscle relaxants work?

A

By reducing the number of nerve conductions from the spinal cord to the PNS

44
Q

What do centrally acting skeletal muscle relaxants NOT interfere with?

A

Nicotinic II receptors

45
Q

What are the CLINICAL INDICATIONS for CNS skeletal muscle relaxants?

A
  1. Muscle Strain
  2. Muscle Injury
  3. Muscle Spasciticy
46
Q

What is the MOA for peripherally acting skeletal muscle relaxants?

A
  1. block N2 receptors at the NMJ from ACH binding to stimulate
  2. interfere with biochemical pathways dealing with actin/myosin
47
Q

What are the 3 classifications of peripherally acting skeletal muscle relaxants?

A
  1. Depolarizing (succinylcholine, IV only MOA #1)
  2. Non-depolarizing (tubocurarine, metocurine, pipecuronium, all = MOA #1)
  3. Direct Acting (dantrolene, PO only, MOA #2)
48
Q

What are the CLINICAL INDICATIONS for PNS skeletal muscle relaxants?

A
Depolarizing/Non-depolarizing
1. Short Surgical Procedures
2. Longer Surgical Procedures w/ abdominal muscles
3. Electroconvulsive Shock Therapy
Direct-Acting
1. Muscle Spastic Diseases
49
Q

What system is stimulated by the binding of ACH to cholinergic receptors?

A
  1. Cholinergic/Muscarinic = Parasympathetic
  2. Cholinergic/Nicotinic I = PNS & SNS
    SNS = mainly heart
    PNS = mainly GI
  3. Cholinergic/Nicotinic II = Somatic
50
Q

Which receptors do ganglionic blocks block?

A

Nicotinic I Receptors (both SNS and PNS)
CI = SEVERE hypertension
Drug = Mecamylamine