1. Prolong Action Potential 2. Shorten Action Potential 3. No Effect on Action Potential

1. Class IA Anti-Arrhythmics 2. Class IB Anti-Arrhythmics 3. Class IC Anti-Arrhythmics

Introduction Flashcards by Mark Agustin

Articles used in diagnosis prevention treatment mitigation of diseases

Drugs

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

Pharmacodynamics

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▪️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)

Pharmacokinetics

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

Pharmacotherapeutics

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CLASSIFICATION OF DRUGS

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

Functional Modifiers

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CLASSIFICATION OF DRUGS

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

Replenishers

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CLASSIFICATION OF DRUGS

Drugs that are used to confirm diagnosis of certain diseases

Diagnostic Agents

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CLASSIFICATION OF DRUGS

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

Chemotherapeutic Agents

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

Target Protein Mediated

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Basic unit of the structural protein

Tubulin

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Made of alpha and beta units of tubulin

Microtubules

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Target Protein
Structural Proteins
▪️Target?
▪️Drugs?

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

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DRUGS THAT INHIBIT MICROTUBULES (4)

Griseofulvin
Colchicine
Antimitotic Drugs (Chemo Drugs)
Benzimidazole

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

Colchicine

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

Griseofulvin

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Neurotoxic

Vincristine (under Vinca Alkaloid as Antimitotic/AntiCA Drugs)

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Taxanes (Under Antimitotic/AntiCA Drugs)

Paclitaxel
Docetaxel
Cabazitaxel

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

Regulatory Proteins

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

Voltage-Gated Na-Channels

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

Voltage-Gated K Channels

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

Disopyramide
Quinidine
Procainamide

Class IA Anti-arrhythmics

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

Tocainamide
Mexiletine
Lidocaine
Phenytoin

Class IB Anti-arrhythmics

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

Moricizine
Flecainide
Propafenone
Encainide

Class IC Anti-arrhythmics

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Prolong Action Potential
Shorten Action Potential
No Effect on Action Potential

Class IA Anti-Arrhythmics
Class IB Anti-Arrhythmics
Class IC Anti-Arrhythmics

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

Ca Channel Blockers

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

Class II Anti-Arrhythmics

What Class Number of Anti-Arrhythmics are the ff. drugs: Mnemonics: BBIDAS Bepridil Bretylium Ibutilide Dofetilide Amiodarone Sotalol

Class III Anti-Arrhythmics

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

Class IV Anti-Arrhythmics

CARRIER MOLECULES (2)

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

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

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

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

H/K-ATPase Pump (Proton Pump)

Enzymes (Under Regulatory Proteins) Inhibited by NSAIDs, Aspirin, -coxibs

Cyclooxygenase (COX)

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

COX-1

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

COX-2

Withdrawn in the market due to myocardial infraction (MI)

Rofecoxib

Enzymes (Under Regulatory Proteins) Inhibitors: MAOI A & B Selective, Non-Selective

Monoamine oxidase (MAO)

What are MAOIs Mnemonics: MPITS

Moclobemide Phenelzine Isocarboxazid Tranylcypromine Selegiline

Selective MAOI A (1)

Moclobemide

Selective MAOI B (2)

Selegine Rosagiline

Non-Selective MAOI

Phenelzine Isocarboxazid Tranylcypromine

Metabolizes: NE, EPI, 5-HT3

MAO A

Metabolizes: Dopamine

MAO B

Diseases: ▪️↓NE ▪️↓5-HT

Clinical Depression

Diseases: ▪️↓Dopamine

Parkinsonism

Enzymes (Under Regulatory Proteins) Inhibitor: Zileuton (Anti-asthma)

5-lipoxygenase (5-LOX)

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

Phospholipids

For cycloprotection, pain, inflammation

Prostaglandin

For bronchoconstriction

Leukotrienes

Enzymes (Under Regulatory Proteins) Inhibitors: ▪️COMTIs "-capones" ▪️ Tolcapone ▪️ Entacapone

Catechol-O-methyltransferase (COMT)

Regulatory Proteins ▪️Channels (3)

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

Regulatory Proteins ▪️Carrier Molecules (2)

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

Regulatory Proteins ▪️Enzymes (6)

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

DRUG-TARGET PROTEIN MEDIATED MECHANISM OF ACTION Receptors (4)

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

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)

Type I Ionotropic Receptors

Examples of Type I Ionotropic Receptors (2)

1.GABA Receptor Complex 2. Nicotinic Receptors

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

GABA Complex

GABA A Receptor Stimulators: (2 B)

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

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

Nicotinic Receptors

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

Ondasetron

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

Type II Metabotropic Receptors

G-Receptors/ANS ▪️Under Gq (4)

1. a1 2. M1 3. H1 4. V1

G-Receptors/ANS ▪️Under Gi (3)

1. a2 2. M2 3. Dopa 2

G-Receptors/ANS ▪️Under Gs (5)

1. B1 2. B2 3. Dopa 1 4. H2 (Histamine) 5. V2 (Vasopressin)

1. (-triptans) -> for migraine 2. Ergot Alkaloids 3. (-setrons) bind to Anti-emetics

1. 5-HT1D 2. 5-HT2 3. 5-HT3

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

What Beta Type Receptors 1. HEART 2. LUNGS

1. B1 Receptors (Heart) 2. B2 Receptors (Lungs)

SABA or LABA? ▪️Salbutamol ▪️Albuterol ▪️Terbutaline

SABA

SABA or LABA? ▪️Salmeterol ▪️Formoterol

LABA

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

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

QISS-QIQ-SIQ-SQS Receptors Mnemonics: Kiss & kick till you're sick of sex

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

In what body fluid is prostaglandin derive?

Semen

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

Type III Enzyme-Linked Receptors

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

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

DRUG-TARGET PROTEIN MEDIATED MECHANISM OF ACTION (Receptors) MOA 1. Depolarization (Na, Ca) & Hyperpolarization (K, Cl) 2. 2° Messenger 3. Phosphorylation 4. Gene Expression

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

NON-TARGET PROTEIN MEDIATED MECHANISM (3)

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

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

Colligative Mechanism/Mass Effect

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

Chemical Antagonism /Direct Chemical Rxn

Systemic Antacids ▪️NaHCO3 ▪️NH4Cl

▪️Metabolic Acidosis ▪️Metabolic Alkalosis

For Heparin Toxicity

Protamine Sulfate

For Wilson's Disease (Cu poisoning)

Penicillamine (Cuprimine°)

For Fe3+ or hemochromatosis

Deferoxamine (Desferal°)

For Hg & As toxicity (peanut oil as vehicle)

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

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

Counterfeit/Incorporation Mechanism

Cornerstone in colon CA chemotherapy

5-FU