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M4: Pharmacology-Pharmacokinetics > Introduction > Flashcards

Introduction Flashcards

1
Q

Articles used in diagnosis prevention treatment mitigation of diseases

A

Drugs

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2
Q

▪️What the DRUG does to the BODY
▪️ Study of the biochemical and physiological effects of drugs
▪️Effects (MOA)

A

Pharmacodynamics

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3
Q

▪️What the BODY does to the DRUG
▪️ Study of processes a drug undergoes as it reaches and leaves the biological site of action
▪️Fate & Disposition (ADME)

A

Pharmacokinetics

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4
Q

▪️ Study of rational use of drugs in the management of diseases
▪️Clinical & Uses

A

Pharmacotherapeutics

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5
Q

CLASSIFICATION OF DRUGS

▪️ Drugs that alter the biochemical and physiological functions of the cell
▪️Biggest Class of Drugs

A

Functional Modifiers

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6
Q

CLASSIFICATION OF DRUGS

Add/Supplement endogenous compounds which are insufficient/lacking/absent

A

Replenishers

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7
Q

CLASSIFICATION OF DRUGS

Drugs that are used to confirm diagnosis of certain diseases

A

Diagnostic Agents

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8
Q

CLASSIFICATION OF DRUGS

Agents used to kill or inhibit growth cells considered as foreign to the body

A

Chemotherapeutic Agents

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9
Q

▪️Biologic site of action, “action site” or “active site”
▪️Targets a physiologic action
▪️Ex. Structural & Regulatory Proteins

A

Target Protein Mediated

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10
Q

Basic unit of the structural protein

A

Tubulin

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11
Q

Made of alpha and beta units of tubulin

A

Microtubules

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12
Q

Target Protein
Structural Proteins
▪️Target?
▪️Drugs?

A

▪️Target: Tubulin, Microtubules
▪️Drugs: Griseofulvin, Colchicine, Vinca, Taxanes

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13
Q

DRUGS THAT INHIBIT MICROTUBULES (4)

A
  1. Griseofulvin
  2. Colchicine
  3. Antimitotic Drugs (Chemo Drugs)
  4. Benzimidazole
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14
Q

▪️1st line tx for acute gout
▪️Inhibits chemotaxis of immune cells that causes inflammation

A

Colchicine

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15
Q

▪️Antifungal agent for Dermatophytosis (tinea/ringworm)
▪️Enzyme inducer
▪️Inhibit blocks fungal mitosis

A

Griseofulvin

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16
Q

Neurotoxic

A

Vincristine (under Vinca Alkaloid as Antimitotic/AntiCA Drugs)

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17
Q

Taxanes (Under Antimitotic/AntiCA Drugs)

A

Paclitaxel
Docetaxel
Cabazitaxel

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18
Q

▪️Regulates biochemical or physiological cell activity or function
▪️Ex. Voltage-Gated Ion Channels (Na, K, Ca)

A

Regulatory Proteins

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19
Q

REGULATORY PROTEINS
▪️Class I Anti-Arrhythmics
▪️Local Anesthetics (-caine)
▪️Some Anticonvulsants (Phenytoin, Carbamazepine)

A

Voltage-Gated Na-Channels

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20
Q

REGULATORY PROTEINS
▪️Class III Anti-Arrythmics (BBIDAS)
▪️Insulin Secretagogues (Sulfonylureas: Glimeperide)

A

Voltage-Gated K Channels

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21
Q

What Class Number of Anti-Arrhythmics are the ff. drugs:

Disopyramide
Quinidine
Procainamide

A

Class IA Anti-arrhythmics

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22
Q

What Class Number of Anti-Arrhythmics are the ff. drugs:

Tocainamide
Mexiletine
Lidocaine
Phenytoin

A

Class IB Anti-arrhythmics

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23
Q

What Class Number of Anti-Arrhythmics are the ff. drugs:

Moricizine
Flecainide
Propafenone
Encainide

A

Class IC Anti-arrhythmics

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24
Q
  1. Prolong Action Potential
  2. Shorten Action Potential
  3. No Effect on Action Potential
A
  1. Class IA Anti-Arrhythmics
  2. Class IB Anti-Arrhythmics
  3. Class IC Anti-Arrhythmics
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25
Q

REGULATORY PROTEIN-CHANNELS?
▪️Dihydropyridine “-dipines”
▪️Non-DHP Class IV Anti-Arrhythmics
▪️ Ex. Verapamil - cardioselective tx for arrhythymia; Diltiazem

A

Ca Channel Blockers

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26
Q

What Class Number of Anti-Arrhythmics are the ff. drugs:

Propranolol
Esmolol
Acebutolol

A

Class II Anti-Arrhythmics

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27
Q

What Class Number of Anti-Arrhythmics are the ff. drugs:

Mnemonics: BBIDAS
Bepridil
Bretylium
Ibutilide
Dofetilide
Amiodarone
Sotalol

A

Class III Anti-Arrhythmics

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28
Q

What Class Number of Anti-Arrhythmics are the ff. drugs:

Diltiazem
Verapamil

A

Class IV Anti-Arrhythmics

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29
Q

CARRIER MOLECULES (2)

A
  1. Na/K-ATPase Pump (Na-K Pump)
  2. H/K-ATPase Pump (Proton Pump)
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30
Q

CARRIER MOLECULES
▪️ found in cardiac myocytes
▪️ responsible for Ca extrusion (for contraction)
▪️Inhibitor: Cardiac Glycosides
Digoxin - Digitalis lanata
DigiToxin - Digitalis purpurea

A

Na/K-ATPase Pump (Na-K Pump)

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31
Q

CARRIER MOLECULES
▪️seen in parietal cells at the stomach
▪️HCl production
▪️Inhibitor: PPIs (-prazole)
Omeprazole -most effective in hyperacidity

A

H/K-ATPase Pump (Proton Pump)

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32
Q

Enzymes (Under Regulatory Proteins)

Inhibited by NSAIDs, Aspirin, -coxibs

A

Cyclooxygenase (COX)

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33
Q

What type of cyclooxygenase (COX) is CONSTITUTIVE enzyme responsible for platelet aggregation and gastric protection or stomach/intestine

A

COX-1

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34
Q

What type of cyclooxygenase (COX) is INDUCIBLE enzyme responsible for pain and inflammation

A

COX-2

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35
Q

Withdrawn in the market due to myocardial infraction (MI)

36
Q

Enzymes (Under Regulatory Proteins)

Inhibitors: MAOI A & B Selective, Non-Selective

A

Monoamine oxidase (MAO)

37
Q

What are MAOIs
Mnemonics: MPITS

A

Moclobemide
Phenelzine
Isocarboxazid
Tranylcypromine
Selegiline

38
Q

Selective MAOI A (1)

A

Moclobemide

39
Q

Selective MAOI B (2)

A

Selegine
Rosagiline

40
Q

Non-Selective MAOI

A

Phenelzine
Isocarboxazid
Tranylcypromine

41
Q

Metabolizes: NE, EPI, 5-HT3

42
Q

Metabolizes: Dopamine

43
Q

Diseases:
▪️↓NE
▪️↓5-HT

A

Clinical Depression

44
Q

Diseases:
▪️↓Dopamine

A

Parkinsonism

45
Q

Enzymes (Under Regulatory Proteins)

Inhibitor: Zileuton (Anti-asthma)

A

5-lipoxygenase (5-LOX)

46
Q

Enzymes (Under Regulatory Proteins)

Precursor for Arachidonic Acid, in turn giving prostaglandins and leukotrienes (eicosanoids), with the action of COX and LOX respectively

A

Phospholipids

47
Q

For cycloprotection, pain, inflammation

A

Prostaglandin

48
Q

For bronchoconstriction

A

Leukotrienes

49
Q

Enzymes (Under Regulatory Proteins)

Inhibitors:
▪️COMTIs “-capones”
▪️ Tolcapone
▪️ Entacapone

A

Catechol-O-methyltransferase (COMT)

50
Q

Regulatory Proteins

▪️Channels (3)

A

1.Voltage-Gated Na Channels
2. Voltage-Gated K Channels
3. Ca Channel Blockers

51
Q

Regulatory Proteins

▪️Carrier Molecules (2)

A
  1. Na-K-ATPase Pump
  2. H/K-ATPase Pump (Proton Pump)
52
Q

Regulatory Proteins

▪️Enzymes (6)

A
  1. Eicosanoid Pathway
  2. COX
  3. Angiotensin-Converting Enzymes (ACE) - inhibited by (-prils) for HTN
  4. MAO
  5. Acetylcholinesterase (AChE) - inhibitor: Edrophonium
  6. COMT
53
Q

DRUG-TARGET PROTEIN MEDIATED MECHANISM OF ACTION

Receptors (4)

A
  1. Type I (Ionotropic)
  2. Type 2 (Metabotropic)
  3. Type 3 (Enzyme/Kinase-Linked)
  4. Type 4 (Gene Transcription-Linked)
54
Q

DRUG-TARGET PROTEIN MEDIATED MECHANISM OF ACTION (Receptors)

▪️Loc: Cell Membrane
▪️Onset: Milliseconds (ms)
▪️Mechanism: Binding of ligand to receptors associated with ion channels (Ligand Gated Ion Channels)

A

Type I Ionotropic Receptors

55
Q

Examples of Type I Ionotropic Receptors (2)

A

1.GABA Receptor Complex
2. Nicotinic Receptors

56
Q

(Under Type I Ionotropic Receptors)
▪️Associated with CI channels -
▪️Inhibitory NT
▪️Facilitates influx of Cl- ions = hyperpolarization

A

GABA Complex

57
Q

GABA A Receptor
Stimulators: (2 B)

A
  1. Benzodiazepines - ↑ FREQUENCY of Cl channel opening
  2. Barbiturates - ↑ DURATION
58
Q

(Under Type I Ionotropic Receptors)
▪️Associated with Na+ channels
▪️Excitatory
▪️Drugs: curare derivatives (-curium, -curonium)
▪️Skeletal Muscle Relaxants

A

Nicotinic Receptors

59
Q

What Drug?
Serotonin blockers: -setron
▪️Tx. for cancer-induced nausea

A

Ondasetron

60
Q

DRUG-TARGET PROTEIN MEDIATED MECHANISM OF ACTION (Receptors)

▪️Loc: Cell Membrane
▪️Onset: Seconds (secs.)
▪️Mechanism: Increase or decrease of secondary messengers
▪️ G-protein linked, couple receptors
▪️ 7-transmembrane spanning receptors

A

Type II Metabotropic Receptors

61
Q

G-Receptors/ANS

▪️Under Gq (4)

A
  1. a1
  2. M1
  3. H1
  4. V1
62
Q

G-Receptors/ANS

▪️Under Gi (3)

A
  1. a2
  2. M2
  3. Dopa 2
63
Q

G-Receptors/ANS

▪️Under Gs (5)

A
  1. B1
  2. B2
  3. Dopa 1
  4. H2 (Histamine)
  5. V2 (Vasopressin)
64
Q
  1. (-triptans) -> for migraine
  2. Ergot Alkaloids
  3. (-setrons) bind to Anti-emetics
A
  1. 5-HT1D
  2. 5-HT2
  3. 5-HT3
65
Q

What Type of G-Proteins is?
▪️ Stimulates adenylyl cyclase (AC)
▪️ Increase cAMP
▪️Stimulators: Epi, NE
▪️Ex. Beta-blockers

66
Q

What Beta Type Receptors
1. HEART
2. LUNGS

A
  1. B1 Receptors (Heart)
  2. B2 Receptors (Lungs)
67
Q

SABA or LABA?

▪️Salbutamol
▪️Albuterol
▪️Terbutaline

68
Q

SABA or LABA?

▪️Salmeterol
▪️Formoterol

69
Q

What Type of G-Proteins is?
▪️ Inhibits adenylyl cyclase (AC)
▪️ Decrease cAMP
▪️Pre-synaptic Alpha 2 receptors
▪️Stimulators: Clonidine, Guanfacine, Guanabenz, Methyldopa
▪️Inhibitor: Yohimbine

70
Q

What Type of G-Proteins is?
▪️Stimulates Phospholipase C (PLC)
▪️PLC stimulates the formation of IP3 & DAG
▪️Increase Ca ions=contraction
▪️Ex. Alpha 1, M1, M3, Post-synaptic a2 receptors

71
Q

QISS-QIQ-SIQ-SQS Receptors

Mnemonics:
Kiss & kick till you’re sick of sex

A

QISS - Alpha 1,2 & Beta 1,2
QIQ - M1, M2, M3
SIQ - D1, D2, H1
SQS - H2, V1, V2

72
Q

In what body fluid is prostaglandin derive?

73
Q

DRUG-TARGET PROTEIN MEDIATED MECHANISM OF ACTION (Receptors)

▪️Loc: Cell Membrane
▪️Onset: Minutes (min.)
▪️Mechanism: Direct binding of ligand to particular receptors / Phosphorylation
▪️ Insulin Receptors - Tyrosine Kinase Linked [Effects: Stimulation of glucokinase]
▪️ Ex: Platelet-derived Growth Factor, Epidermal Growth Factor

A

Type III Enzyme-Linked Receptors

74
Q

DRUG-TARGET PROTEIN MEDIATED MECHANISM OF ACTION (Receptors)

▪️Loc: Cytoplasm/Nucleus
▪️Onset: Hours (hrs.)
▪️Mechanism: Modulate Gene Transcription
▪️Ex: Steroid Hormones, Thyroid Hormones, Vit. D & Derivative

A

Type IV Gene Transcription-linked Receptor/Nuclear Receptor/Intracellular Receptor

75
Q

DRUG-TARGET PROTEIN MEDIATED MECHANISM OF ACTION (Receptors)

MOA
1. Depolarization (Na, Ca) & Hyperpolarization (K, Cl)
2. 2° Messenger
3. Phosphorylation
4. Gene Expression

A
  1. Type 1Ionotropic
  2. Type 2 Metabotropic
  3. Type 3 Enzyme-linked
  4. Type 4 Gene Transcription-linked
76
Q

NON-TARGET PROTEIN MEDIATED MECHANISM (3)

A
  1. Colligative Mechanism/Mass Effect/Physical Interaction
  2. Chemical Antagonism/Direct Chemical Interaction
  3. Counterfeit or Incorporation Mechanism
77
Q

NON-TARGET PROTEIN MEDIATED

▪️Colligative Properties - dependent on the number of solute particles in a solution
▪️Mannitol - osmotic diuretic/aquaretic

A

Colligative Mechanism/Mass Effect

78
Q

NON-TARGET PROTEIN MEDIATED

▪️Acid-Base Neutralization
● Local Antacids
- Neutralization Rxn
(Ex. Mg(OH)2, Al(OH)3, CaCO3)
▪️Chelation/Complexation (Heavy Metal + Antidote)

A

Chemical Antagonism /Direct Chemical Rxn

79
Q

Systemic Antacids
▪️NaHCO3
▪️NH4Cl

A

▪️Metabolic Acidosis
▪️Metabolic Alkalosis

80
Q

For Heparin Toxicity

A

Protamine Sulfate

81
Q

For Wilson’s Disease (Cu poisoning)

A

Penicillamine (Cuprimine°)

82
Q

For Fe3+ or hemochromatosis

A

Deferoxamine (Desferal°)

83
Q

For Hg & As toxicity (peanut oil as vehicle)

A

Dimercaprol (IM) or British Anti-Lewis (BAL)

84
Q

NON-TARGET PROTEIN MEDIATED

▪️Aka: Drug Incorporation
▪️ Ex: Antimetabolites
▪️Purine and pyrimidine base analogues (also used as AntiCA drugs-Flucytosine)

A

Counterfeit/Incorporation Mechanism

85
Q

Cornerstone in colon CA chemotherapy

M4: Pharmacology-Pharmacokinetics (50 decks)

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