Comprehensive Pharmacology Lecture Review

Comprehensive practice flashcards covering basic pharmacology principles, pharmacokinetics, pharmacodynamics, autonomic drugs, hematologics, and cardiovascular treatments based on clinical lecture notes.

How is Pharmacology defined in the notes?

The study of drugs, including their effects (MOA), fate and disposition (ADME), and clinical uses (indications).

What are the two main branches of Pharmacology?

Pharmacodynamics (drug effects on the body) and Pharmacokinetics (body's effect on the drug).

What are the three purposes of drugs according to the lecture?

Mitigation, diagnosis (dx), and prevention or treatment (Tx) of cure.

What is the difference between Levothyroxine and Dextrothyroxine?

Levothyroxine is the preparation of choice and is $14\times$ more potent than Dextrothyroxine, which only has $44129$ of the activity of the Levo form.

Which drug is used for Central Diabetes Insipidus?

Vasopressin.

How is Afrezza administered and what is its use?

It is an inhalational insulin used for the treatment of Type 1 Diabetes Mellitus (T1DM).

Identify the diagnostic use and effect of Methacholine.

It is used in the Pulmonary Challenge Test as it causes bronchoconstriction.

What is the function of Edrophonium in the Tensilon Test?

It is an anticholinesterase that increases muscle strength to diagnose Myasthenia Gravis.

What are Chemotherapeutic Agents?

Agents that kill or limit the growth of foreign cells (bacteria, viruses, fungi) or cancer cells (antineoplastics).

What drugs inhibit microtubules during mitosis?

Taxanes (Paclitaxel), Vinca alkaloids, and Griseofulvin (antifungal).

What is the first-line treatment for acute gout mentioned in the notes?

Colchicines, which inhibit tubulin polymerization but are not hypouricemic.

Give examples of Sodium ($Na^+$) channel blockers and their effects.

Anticonvulsants (Carbamazepine, Phenytoin), Local Anesthetics (ending in -caine), and Class I Antiarrhythmics; they inhibit depolarization.

What is the mechanism and use of Digoxin?

It inhibits the $Na^+-K^+$ ATPase Pump, increasing intracellular $Ca^{2+}$ for positive inotropic effects in Congestive Heart Failure (CHF).

How do SGLT2 inhibitors like Dapagliflozin work?

They inhibit the $Na^+$-glucose-linked transporter 2 in the kidneys (PCT) to prevent glucose reabsorption, used in T2DM.

Contrast the selectivity of MAO inhibitors Moclobemide and Selegiline.

Moclobemide is $MAO_A$-selective, while Selegiline is $MAO_B$-selective.

What are the four types of Receptors based on onset and location?

Type I: Ionotropic (milliseconds); Type II: G-Protein Coupled (seconds); Type III: Kinase-linked (minutes); Type IV: Gene transcription linked/Nuclear (hours).

What is the effect and poisoning associated with Glycine receptors?

They cause hyperpolarization (inhibitory); Strychnine is a competitive antagonist (tetanic poison).

Identify the G-protein types and their messengers.

$G_s$ (+ adenylyl cyclase, $↑ cAMP$), $G_i$ (- adenylyl cyclase, $↓ cAMP$), and $G_q$ (+ PLC, $↑ IP_3$ and DAG).

What is Mannitol's mechanism of action?

Physical interaction via colligative properties/osmosis; acts as a cathartic (PO) or a diuretic (IV).

What is the difference between an Agonist and an Antagonist regarding Intrinsic Activity (IA)?

Agonists have affinity and IA ($>0$), while Antagonists have affinity only ($IA = 0$).

What is the first-line treatment for Anaphylactic Shock?

Epinephrine (EPI).

Explain the difference between Competitive and Non-Competitive Antagonism surmountability.

Competitive is surmountable by increasing the agonist dose (rightward shift on log-dose curve); Non-competitive is not completely surmountable (lower height/efficacy).

Define Potency ($P$).

The dose required to achieve $504129$ of efficacy ($ED_{50}$).

What is the formula for the Therapeutic Index ($TI$)?

$TI = \frac{TD_{50}}{ED_{50}}$, where a higher value indicates a safer drug.

State Fick's Law of Diffusion.

$\frac{dQ}{dt} = \frac{D \times A \times k \times (C_{G1} - C_p)}{h}$.

What are the terms 'LUNA' and 'HIPE' used to describe in drug absorption?

LUNA: Lipophilic Unionized Non-polar Absorbed (occurs when drug and environment pH match); HIPE: Hydrophilic Ionized Polar Excreted (occurs when they differ).

What equation governs the rate of drug dissolution?

The Noyes-Whitney Equation.

What is the Bioavailability ($F$) formula for an extravascular dose?

$F_{abs} = \frac{AUC_{PO}}{AUC_{IV}}$.

Distinguish between Pharmaceutical Equivalents and Pharmaceutical Alternatives.

Equivalents have the same API, strength, and DF; Alternatives have the same API but may differ in salt, ester, strength, or DF.

How does protein binding affect drug activity?

Bound drugs are inactive and stay in the blood; free drugs are active and can distribute to tissues ($↑ V_D$).

What is a prodrug? Give examples from the notes.

An inactive drug that becomes active through metabolism; examples include ACEIs (ex: Enalapril to Enalaprilat) and Clopidogrel.

Identify the toxic metabolite of Acetaminophen (APAP).

NAPQI, which is hepatotoxic and neutralized by N-acetylcysteine (NAC).

What is the First-Pass Effect (FPE)?

Initial metabolism of a drug in the small intestine or liver prior to reaching systemic circulation, reducing oral bioavailability.

What causes Gray Baby Syndrome?

Chloramphenicol use in neonates due to deficient Glucuronidation (Phase 2 metabolism).

Compare SANS and PANS origin and neurotransmitters.

SANS: Thoracolumbar ($T_1 - L_2$), uses NE at post-ganglion; PANS: Craniosacral (CN 3, 7, 9, 10, $S_2 - S_4$), uses ACh at post-ganglion.

Name the rate-limiting enzyme in Norepinephrine (NE) synthesis.

Tyrosine Hydroxylase.

What is the major route of Termination for Norepinephrine (NE)?

Reuptake via the NE Transporter (uptake-1).

What is the effect of $\beta_2$ receptor activation on the lungs and uterus?

Bronchodilation in the lungs and Tocolysis (relaxation) in the uterus.

Identify the side effects of Methyldopa.

Sedation, depression, hepatotoxicity, and a positive Coombs test (hemolytic anemia).

What is the 'First Dose Phenomenon' and which drug class causes it?

Orthostatic hypotension and syncope occurring after the first dose of ̑_1-selective blockers (e.g., Prazosin).

Which Beta Blocker is considered the most cardioselective?

Nebivolol.

List the components of SLUDGE or DUMBBELICS toxicity for cholinomimetics.

Diarrhea, Urination, Miosis, Bronchoconstriction, Bradycardia, Emesis, Lacrimation, Salivation, and Sweating.

What are the common antidotes for Organophosphate poisoning?

Atropine (antimuscarinic) and Pralidoxime (cholinesterase regenerator, if used within $48$ hours).

What is the antidote for Malignant Hyperthermia caused by Succinylcholine?

Dantrolene.

How is Heparin activity monitored, and what is its antidote?

Monitored via aPTT; the antidote is Protamine Sulfate ($1\text{ mg protamine per 100 U heparin}$).

What enzyme does Warfarin inhibit to prevent clotting?

Vitamin K Epoxide Reductase Complex ($VKORC$), preventing the synthesis of factors II, VII, IX, and X.

What is the diagnostic marker for monitoring Warfarin?

PT-INR ($goal = 2.0 - 3.0$ for most, $2.5 - 3.5$ for prosthetic valves).

What is the mechanism and primary side effect of Statins?

They inhibit HMG-CoA Reductase (blocking de-novo cholesterol synthesis); side effects include hepatotoxicity and Rhabdomyolysis.

How does Ezetimibe work to lower cholesterol?

It inhibits the Niemann-Pick C1-Like 1 ($NPC1L1$) transporter, blocking cholesterol absorption.

What is the cardinal sign of Niacin (Nicotinic Acid) side effects, and how is it managed?

Erythema (flushing); managed by taking low-dose Aspirin ($ASA$) or Ibuprofen.

Distinguish between Osteoarthritis (OA) and Rheumatoid Arthritis (RA).

OA is non-inflammatory; RA is an autoimmune inflammatory condition characterized by symmetrical joint involvement and morning stiffness ($>1\text{ hour}$).

Which drug is used as a 'rescue drug' for Methotrexate ($MTX$) toxicity?

Folinic acid (Leucovorin).

Identify the primary enzymes in uric acid metabolism and their inhibitors.

Xanthine Oxidase (inhibited by Allopurinol and Febuxostat) and Urate Oxidase (Pegloticase is a recombinant form).

Trace the Renin-Angiotensin-Aldosterone System ($RAAS$) pathway.

Angiotensinogen (liver) $\rightarrow$ Angiotensin I (via Renin) $\rightarrow$ Angiotensin II (via ACE).

What is the primary site of action for Loop Diuretics?

The Thick Ascending Limb ($TAL$) of the Loop of Henle ($LOH$).

Identify the unique electrolyte side effect of Thiazide diuretics.

Hypercalcemia ($Ca^{2+}$ is saved), unlike Loop diuretics which cause hypocalcemia.

What is the mechanism and unique side effect of Spironolactone?

It is an Aldosterone antagonist and K-sparing diuretic; side effects include Gynecomastia and loss of libido due to its antiandrogenic properties.

Which Calcium Channel Blocker ($CCB$) is the most cardioselective?

Verapamil.

What are the common side effects of ACE inhibitors?

Dry cough and angioedema (due to Bradykinin accumulation), hyperkalemia, and hypotension.

What is 'Monday Disease' in the context of Nitrates?

Tolerance to the vasodilating effects of organic nitrates that develops with continuous use.

What is the primary sign of Digoxin toxicity vision changes?

Yellow-green discoloration (Xanthopsia).

What are the four classes of antiarrhythmics in the Vaughan Williams system?

Class I: Sodium channel blockers; Class II: Beta blockers; Class III: Potassium channel blockers; Class IV: Calcium channel blockers.

Name the first-line treatment for Torsades de Pointes.

Magnesium Sulfate ($MgSO_4$).

Identify the primary source of Opiates.

Papaver somniferum.

What is the diagnostic triad for Narcotic poisoning and the antidote?

Miosis, respiratory depression, and coma; the antidote is Naloxone.

Which opioid is used for smoking cessation as a partial agonist?

Varenicline (though the notes also mention Lobeline).