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Digestive Systems, Nutrition, & Metabolism > Drugs > Flashcards

Drugs Flashcards

1
Q

Amytal (Amobarbital)

A
  • Reversible Inhibitor of Complex I (NADH Dehydrogenase)
    • Blockade of ETC with Amytal has been shown to protect cardiac muscle during ischemia-reperfusion by limiting ROS production
      ○ Protective against ROS accumulation
    • Still will make some ATP via Complex II and BYPASS REACTIONS (via Succinate DH –> FADH2)
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2
Q

Rotenone

A
  • Inhibits Complex I (NADH Dehydrogenase)
    • Naturally occurring pesticide
    • Fish poison
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3
Q

Antimycin

A
  • Inhibits Complex III
    ○ Binds to cytochrome b in the reduced state –> stops ETC
    ○ Inhibits BOTH BYPASS AND NON-BYPASS REACTIONS (because it’s beyond complex II)
    § Complexes I, CoQ, + Complex II: fully reduced
    § Complexes III, Cytochrome C, + Complex IV: fully oxidized because no electron transport can occur here and beyond
    • Antifungal: agricultural use
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4
Q

Cyanide

A
  • Inhibits Complex IV
    ○ CN binds to oxidized form of Heme Iron (Ferric: Fe 3+) –> prevents Complex IV from being reduced!
    • Treatment for Cyanide Poisoning:
      ○ Nitrite (NO2-) followed by Thiosulfate (S2O3)
      § Nitrate: Hemoglobin + Nitrite –> Met-Hb (Fe3+) –> Met-Hb competes for binding of CN to Complex IV–> CN-Met-Hb (Fe3+)
      § Thiosulfate: Thiosulfate –> reacts with CN – SCN (Thiocyanate) + SO3 –> excreted urine
      □ Thiocyanate is less toxic and more hydrophilic –> excreted in urine
      ○ Thiosulfate can also work on its own
      § Thiosulfate + CN –> via Rhodanese enzyme (endogenous) –> SCN (Thiocyanate) + SO3 –> Urine
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5
Q

Oligomycin

A
  • Inhibits Fo portion of ATP Synthase:
    • Blocks proton flow through Fo –> prevents reentry of protons into mitochondrial matrix
    • NO ATP MADE
    • Proton gradient builds up
    • Electron transport will soon stop because of the difficulty of pumping protons against a VERY steep proton gradient –> inhibition of ATP formation by Oligomycin also prevents oxidation reduction reactions
    • Used in the lab
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6
Q

AraC

A

cancer treatment

- Damage the inner mitochondrial membrane: dissipates proton flow so it goes back into matrix

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7
Q

AZT

A

used as HIV treatment

- Damage the inner mitochondrial membrane: dissipates proton flow so it goes back into matrix

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8
Q

Aspirin

A
  • Kidnaps protons within intermembrane space –> cross inner membrane –> into matrix
    ○ Able to do this because it is very LIPID SOLUBLE and weak base
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9
Q

DNP (Dinitrophenol) high dose

A
  • Kidnaps protons within intermembrane space –> cross inner membrane –> into matrix
    ○ Able to do this because it is very LIPID SOLUBLE and weak base
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10
Q

Atratyloside

A
  • Inhibits ADP/ATP Antiporter (ATP/ADP Translocase)
    • Prevents transport and availability of ADP in the matrix for ATP synthesis –> stops ATP synthesis
    • Atractyloside Poisoning occurs in Mediterranean area and Northern Africa:
      ○ Atractylis gummifera L:
      § Easily confused with wild artichoke
      § Children eat because sweet tasting and roots like chewing gum
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11
Q

Disulfarim

A
  • Inhibits Acetaldehyde Dehydrogenase activity
    • Causes unpleasant effects when even small amounts of alcohol are consumed
      ○ Unpleasant effects due to ↑acetaldehyde
    • Discourages drinking but not a cure for alcoholism
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12
Q

NAPQI (N-Acetylbenzoquinonemine)

A
  • metabolite of Tylenol (Acetaminophen) by MEOS system
  • chronic heavy drinks who are sober: CYP activity is enhanced. as a result, the metabolism of Tylenol is enhanced –> increase in NAPQI –> LIVER DAMAGE
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13
Q

Phenytoin

A
  • Inhibits Folate Conjugase (Expressed on jejunum epithelium)
  • prevents conversion of polyglutamate folate –> monoglutamate folate
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14
Q

Methotrexate

A
  • COMPETITIVE INHIBITOR of DHFR
  • prevents conversion of Folate –> DHF –> THF
  • chemotherapeutic
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15
Q

Aminopterin

A
  • Inhibits DHFR
  • prevents conversion of Folate –> DHF –> THF
  • chemotherapeutic*
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16
Q

Leucovorin (Folinic Acid)

A
  • Bypasses the metabolic block of Methotrexate
  • Bypasses DHFR block of Methotrexate
  • Effective at combating the neurotoxicity, GI toxicity, and myelosuppression effects of Methotrexate
    ○ Folinic Acid is the ACTIVATED form of Folate
17
Q

Sulfonamides

A
  • Inhibits DHPS (Dihydropteroate Synthetase) in bacteria
  • this enzyme is unique to bacteria
  • prevents Folic Acid synthesis in bacteria
18
Q

Trimethoprim

A
  • PREFERENTIALLY inhibits bacteria DHFR (Dihydrofolate Reductase) over human DHFR
  • Prevents THF formation
19
Q

Azaserine

A

Potent inhibitors of purine nucleotide synthesis by irreversibly inhibiting PRPP-amido-transferase
- glutamine analog

20
Q

DON

A

Potent inhibitors of purine nucleotide synthesis by irreversibly inhibiting PRPP-amido-transferase
- glutamine analog

21
Q

Ribavirin

A
  • Inhibits IMP Dehydrogenase
  • Depletes intracellular pools of GUANINE nucleotides
  • antiviral used to treat Hepatitis C
22
Q

Mycophenolic Acid

A
  • Inhibits IMP Dehydrogenase
  • Depletes intracellular pools of GUANINE nucleotides
  • used as immunosuppressant to prevent graft rejction (renal transplants)
23
Q

Allopurinol

A

Xanthine Oxidase Inhibitor; 3-fold mechanism

	1. Allopurinol --> COMPETITIVELY inhibits Xanthine Oxidase
	2. Allopurinol is converted to Alloxanthine by Xanthine Oxidase
		i. Alloxanthine is a potent IRREVERSIBLE inhibitor of Xanthine Oxidase
		- Xanthine and hypoxanthine are more soluble than uric acid and can be excreted in the urine easily***
	3. Allopurinol --> ↓Xanthine Oxidase --> ↑Hypoxanthine --> salvaged to produce IMP
		i. IMP is an INHIBITOR of PRPP-Amido-Transferase --> ↓purine synthesis and thus ↓purine degradation
  • used for GOUT treatment
  • hypoxanthine analog
24
Q

Hydroxyurea

A

Inhibitor of Ribonucleotide Reductase

- used as a cancer treatment

25
Q

5-Fluorouracil

A
  • Gets converted to 5-FdUMP by Thymidine Kinase
    • 5-FdUMP covalently inhibits Thymidylate Synthase
    • Leads to THYMINELESS CELL DEATH
  • used an cancer treatment
26
Q

Acyclovir

A
  • used to treat Herpes Simplex Virus
  • phosphorylated by viral Thymidine Kinase
  • (P)-Acyclovir then acts as a DNA chain terminator
  • Guanosine Analog
27
Q

Sovaldi

A
  • used to treat Hepatitis C
  • Uridine analog
  • obligate chain terminator
28
Q

Bactrim

A

mix of Sulfonamide + Trimethoprim

- inhibits THF production in bacteria

29
Q

Abarcose

A

Inhibits alpha-glucosidases:

- Slows absorption of carbohydrates in the small intestine - ↓postprandial elevations in blood glucose - used for DM 2 - also used to LOWER CHOLESTEROL
30
Q

Sulfonyureas (Gilburide)

A

Inhibits ATP-sensitive K+ channel in B-cells

- ↑K+ intracellular concentration
- Causes longer depolarization of the B-cell membrane
- Longer triggering and opening of voltage-gated Ca channels
- Elicits a RISE in intracellular Ca2+
  • ↑insulin secretion from B-cell
  • ↓serum glucagon levels
  • used for DM 2
31
Q

Metformin (Biguanides)

A

INHIBITS GNG STIMULATES GLYCOLYSIS
- Inhibits complex I of ETC –> ↓ATP production –> ↑AMP –> ↑AMPK
- ↑AMP –> inhibit AC –> ↓cAMP –> ↓PKA –> ↓GNG + ↑Glycolysis
- ↑AMPK –> IMPROVES INSULIN SENSITIVITY:
○ ↑AMPK –> ↑insulin receptor function
○ ↑AMPK –> ↑glucose transport
○ ↑AMPK –> ↓FA synthesis

- Improves insulin sensitivity:
	• ↑insulin receptor function
	• ↑glucose transport
	• ↓FA synthesis
	• ↑Glycolysis
	• ↓GNG
- used for DM 2
32
Q

DPP-4 Inhibitor (Januvia)

A

Inhibits DPP-4 (hydrolase) –> ↑active incretins

  • Enhances insulin secretion due to ↑incretins
  • used for DM 2
33
Q

SGLT2 Inhibitor

A

Block the reabsorption of glucose in the kidney
- ↑glucose secretion in urine
- ↓blood glucose
- But MAY lead to UTI (urinary tract infections)
○ Glucose in the urine may facilitate bacterial overgrowth
- ↓blood glucose
- used for DM 2

34
Q

Thiazolidinedione (Avandia)

A

Activates PPARy transcription factor

- ↑insulin sensitivity of  adipose tissue
- ↑glucose uptake into adipose tissue and muscle
- Leads to WEIGHT GAIN - ↑insulin sensitivity of adipose tissue - ↓blood glucose - used for DM 2
35
Q

Statins

A
  • Inhibits HMGCoA Reductase
  • increases # of LDL receptors on liver
  • decreases LDL
  • lowers cholesterol
36
Q

Ezetimibe

A
  • inhibits absorption of cholesterol at the brush border membrane in the intestinal membrane
  • increases # of LDL receptors on the liver
  • LDL decreases
  • LOWERS CHOLESTEROL
37
Q

Nicotinic Acid (Niacin)

A
  • inhibits mobilization of FFA from peripheral adipose tissue to the liver
  • LDL decreases
  • LOWERS CHOLESTEROL
38
Q

Bile Acid Sequestrants (BAS)

A
  • depletes bile acid pool and disrupts enterohepatic circulation of bile acids, thus increasing bile acid synthesis from cholesterol
  • LDL decreases
  • LOWERS CHOLESTEROL
39
Q

Fibrates

A
  • decreases VLDL
  • increases HDL
  • LOWERS CHOLESTEROL

Digestive Systems, Nutrition, & Metabolism (3 decks)

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