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Biochemistry > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Describe pH drug trapping.

A

pH of stomach acid: 1.4
PH of plasma: 7.4
PH of Colon: 9.0

If the pKa of a drug is less than the pH of the medium you have the charged form.
If the pKa of a drug is more than the pH of the medium you have the uncharged form so it can pass through the lipid bilayer.

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2
Q

What prevents drugs from getting through the blood brain barrier?

A

Tight junctions of the capillaries. If the drug is very hydrophobic it can cross.

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3
Q

What is first pass metabolism?

A

It is the metabolizing of the drug in the liver when absorbed in the bloodstream through the GI system. Lowers the amount of free drugs.

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4
Q

What is Bioavailability?

A

The ratio of the amount of drug that reached systemic circulation over the amount of drug administered. Gives number 0-100

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5
Q

Explain loading dose

A

It is an extra dose of drug at first administration to overcome the effect of the volume of distribution (Vd). The higher the Vd of a drug (storage in different bodily tissue) the higher the loading dose needs to be.

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6
Q

How many half lives does it take to reach steady state?

A

3-5

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7
Q

What is the maintenance dose dependent on?

A

Clearance: metabolism+excretion/amount of drug

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8
Q

Explain the significance of protein bound drug.

A

Drugs that bind with proteins like albumin in the blood are more contained in the blood, and thus have a lower Vd. There isn’t as much free drug, or drug stored in the tissue. You need to be careful that levels of proteins in specific patients stay normal because infections and other events can release drug from proteins which will increase the amount of free drug in the individual and can be toxic.

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9
Q

What does cytochrome P450 do?

A

Phase 1: oxidation/reduction reactions
Phase 2: Conjugation/Hydrolysis reactions
-3 conjugation reactions: glucuronidation, acetylation, sulfation
Happens in LIVER

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10
Q

Explain ED50, LD50, Potency, and Efficacy

A

Effectiveness, different levels of Emax
Potency, different levels of ED50, but get same response curve.
LD50 is Lethal Dose
ED50 is Effective Dose

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11
Q

What is the therapeutic index?

A

An indication for drug safety. The higher the number the safer the drug

LD50/ED50

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12
Q

Explain competitive and non competitive antagonists to drugs.

A

Competitive drugs have no effect on efficacy, and can be overcome by adding more drug.
Non competitive drugs affect the efficacy, and that change in efficacy can’t be overcome by adding more drug.

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13
Q

Describe sensitivity and tolerance

A

Sensitivity is up-Regulation: In the presence of an antagonist the cell can add more drug receptors to accept the drug. If the antagonist leaves the cells reaction to the drug is greater.

Tolerance is down-Regulation: In the presence of an agonist the cell presents less receptors and will need more drug to illicit the same response.

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14
Q

Define additive

A

The effect of drug X and Y are the sum of their two effects.

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15
Q

Define Synergistic

A

The effect of drug X and Y is greater than the sum of their effects alone

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16
Q

Define Tachyphylaxis

A

Decreased drug response by many different factors.

One example is taking a drug too many times and getting used to it. You need to take more to get the same response.

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17
Q

What are the three mechanisms of toxicity

A

Dose Dependent
Dose Independent
Idiosyncratic

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18
Q

What are three examples of Dose dependent toxicity

A

Pharmacological toxicity
Physiological toxicity
Genotoxicity

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19
Q

What does the abbreviation Cp mean?

A

Drug effect

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20
Q

What is the MOS?

A

Margin of Safety

The LD1/ED99

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21
Q

What are 3 considerations that you should take when administering drugs with narrow TI?

A
  1. Monitor the blood levels of the drug
  2. Evaluate the necessity of the drug
  3. Monitor the heath of the organ system.
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22
Q

What are the chemical indicators of Hepatotoxicity?

A 
Jaundice
Increase circulation of hepatic enzymes
-Aspartate aminotransferase
-Alanine aminotransferase
-Alkaline phosphotase
23
Q

What are the chemical indicators of Nephrotoxicity?

A

Decreased Creatinine circulation.

24
Q

Explain the difference between on and off target toxicity effects

A

On target: They affect the same receptor but can be in a different tissue.
Off target: They affect different receptors than intended. (B1 and B2 receptors)

25
Q

What are two specific examples of pathological toxicity

A

Bile Salt Export Protein BSEP: When targeted bile salts can’t leave and the accumulation causes cell necrosis.
Bio transformation of Acetaminophen: CYP2E1 can be used when phase ll enzymes are full. HSG is used to break the toxic metabolite down, but more than 4000 mg/day can use up HSG and cause hepatotoxicity

26
Q

What are five different specific factors that can affect apparent dose?

A
  1. Slower motility
  2. Altered gastric pH
  3. Hypoproteinemia
  4. Reduced Elimination
  5. Impaired Hepatic Function
27
Q

What are two Type 1 Adverse Drug Reactions?

A

Hypersensitivity (Anaphylactics): IgE on Mast cells bind to Antigen or Hapten (drug). Releases Histamine, leukotrines, and serotonin.
Causes: edema, vasodilation, and inflammation

Red Man Syndrome: Mast cells release granules without IgE stimulation
Occurs with intravenous drugs

28
Q

What are type 2 adverse reactions?

A

Cytolytic Reactions (antibody dependent cytotoxic hypersensitivity)
Drug binds to RBC which is then bound IgE or IgM. This results in the Lyse of the RBC.
(Pencillin-induced anemia)

29
Q

What are type 3 adverse reactions?

A

Arthus Reactions (Serum Sickness): Drug is complexed by IgG or IgM in the endothelium of vasculature. This causes the underlying tissue to be destroyed. (Venom)

30
Q

What are type 4 adverse reactions?

A

Delayed hypersensitivity reactions
Inflammation from sensitized T-cells contacting a familiar antigen. Dermitis
Gets worse with 2nd encounter. Can cause cytokine storm.
(Poison Ivy, Latex allergies)

31
Q

What is Stevens-Johnson Syndrome?

A

It is a rare disorder characterized by the necrosis of epidermis from therapeutic drugs. Becomes Toxic Epidural Necrolysis if more than 30% of the body is affected.

32
Q

What neurotransmitters does the sympathetic autonomic system use?

A

Norepinephrine for most effectors
Acetylcholine at ganglia (and some effectors)
Dopamine at some effectors

33
Q

What neurotransmitters does the parasympathetic autonomic system use?

A

Acetylcholine for ganglia and effectors

34
Q

What are the properties of choline esters? Their availability to Acetylcholinesterase and their effects on Nicotinic and Muscarinic receptors?

A

Acetyl Choline: ACEA: ++++ N: +++ M.:+++
Methacholine Chloride: ACEA: + N: ++++ M: None
Carbachol Chloride: ACEA: None N: ++ M: +++
Bethanachol Chloride: ACEA: None N: ++ M: None

35
Q

What are the different subtypes of alkaloid proteins?

A

Tertiary Amines: Affects the CNS (significant GI absorption), Nicotine
Quaternary Amines: Affects only Periphery (charged so stays in blood), muscarinic

36
Q

What are 6 different reasons for Indirect Acting Agents? What do they affect?

A 
(They affect Acetylcholinesterase)
Myasthenia
Post Operative Ileus
Reversal of Neuromuscular Blockade
Pediculosis Capitis
Glaucoma
Urinary Tract Motility
37
Q

What the systemic side effects of direct and indirect parasympathetic drugs?

A

Salivation
Lacrimation
Urination
Deification

38
Q

What are organophosphate?

A

Irreversible Acetylcholinesterase inhibitors

Malathion

39
Q

Why are organophosphates dangerous?

A

With aging one phosphate can be broken which strengthens the bond to the inhibitor and can make inhibition permanent.

40
Q

What are some (8) clinical applications for parasympathetic muscarinic receptors?

A 
Ophthalmology
Cholinergic Poisoning treatment (mushroom)
Parkinson’s Disease
Irrital bowel syndrome
Overactive bladder
Bradycardia
Motion sickness
COPD
41
Q

What is the antidote for mushroom poisoning, and what other compound can you take with it to protect soldiers from organophosphates (nerve gas)?

A

Atropine

Pralidoxime

42
Q

What is the name of the drug for motion sickness, and what other population can take it?

A

Scopolamine

Those who are aging.

43
Q

What is the best antimuscarinic for ophthalmology?

A

Tropicamide

44
Q

What are the best drugs for bladder incontinence and overactive bladder?

A

M3 receptors
Darifenicin
Solifenicin

45
Q

Describe the paradox in treating Brachycardia

A

.5 mg doses of Atropine are effective at speeding the heart (using antimuscarinic), but anything lower than .5 mg can slow the heart more.

46
Q

What is the key in the definition of antimicrobial?

A

Must be created in an organism. Synthesized antimicrobials are not “true”

47
Q

What are challenging areas to get a good MIC/MBC with infections in the body?

A

Site of the infection is in the bone, cns, or adipose

48
Q

What are 5 general resistance mechanisms that bacteria have against antibiotics?

A
  1. Reduce the entry of the drug
  2. Enhance the export of the drug out of the cell
  3. Make enzymes that alter the drug
  4. Change the protein targets of the drug
  5. Change the metabolic or signaling pathways that the drug targets.
49
Q

What are the B-Lactam drugs? What is their target? How are they being resisted against, and what can we do to help that process? What can you take if you have a B-Lactam allergy?

A

Penicillin
Cephalosporins
Carbapenems
Monobactams

They target transpeptidase in the formation of the cell wall. Gram +

Lactamases can be made in the bacteria to open the B-Lactam ring, but if you mix a strong and a weak B-Lactam you can overwhelm the lactamase and allow the strong B-Lactam to fight the infection.

Monobactams are used if there is a B-Lactam allergy (only has two rings

50
Q

What is an example of a glycopeptide drug? What is its target in the bacteria? What is it good against. What can it not kill?

A

Vancomycin
It targets and binds to D-alanine to stop cell wall formation.

It is great against gram +, and especially MRSA

Bacteria can stop using alanine in the cell wall to select against this antibiotic.

CAN’T affect GRAM -

51
Q

What would be affective against vancomycin resistant strains?

What are the two other cell membrane inhibitors?

A

Lipopeptides: Daptomycin

Enters plasma membrane and disrupts concentration of ions.

Bacitracin: Stop subunits of peptidoglycan

Polymyxin: Small + charged
Attack GRAM -

52
Q

What are the indirect inhibitors of DNA synthesis, and what makes them unique

A

Sulfonamides and Trimethoprim

They work synergistically as inhibitors of folic acid synthesis. Sulfonamide targets dihydropteroate synthase and Trimethoprim targets the downstream dihydrofolate reductase.

INDIRECT BACTERIOSTATIC

53
Q

What are 3 protein synthesis inhibitors?

Do they kill bacteria?

A

Erythromycin: prevent translocation of peptide chain

Tetracyclines: Disrupt tRNA interaction with 30S ribosome

Chloramphenicol: Prevent formation of peptide chain.

Have more adverse drug effects.

Mostly BACTERIOSTATIC with som bactericidal exceptions

54
Q

What is an example of Antagonistic drugs?

A

Tetracyclines reducing the efficacy of penicillins.

Bacteriostatic agent with cell wall inhibitor

Biochemistry (6 decks)

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