General Flashcards
Competitive Inhibitors
Mech of Action (3)?
MECH:
- Bind REVERSIBLY to receptor = Bind to receptor’s Active Site
- ↓receptor’s Affinity for substrate =>↑Km
- Can be overcome by↑substrate
Noncompetitive Inhibitors
Mech of Action (2)?
MECH:
- Bind Irreversibly to receptor = Bind to receptor’s Allosteric Site
- ↓Potency =↓Vmax
Drugs that can Cross Barriers (ie BBB, BPB)
Chars (3), Toxicities (3)?
CHARS:
- Uncharged =
- Hydrophobic / Lipophilic
- Basic (usually)
TOX:
- Hepatotoxicity
- CNS symptoms
- Rhabdomyolysis
Metabolized by P450
- RESP Drugs: Methylxanthines (ie Theophylline)
P450 Inducers (7)
- “Barb Steals Phen and Refuses Greasy Carbs Chronically” *
- Barbiturates
- St John’s Wort
- Phenytoin
- Rifampin
- Griseofulvin
- Carbamazepine
- Chronic alcohol abuse
P450 Inhibitors (11)
- “MAGIC RACKS” *
- Macrolides
- Amiodarone
- Grapefruit juice
- Isoniazid
- Cimetidine
- Ritonavir
- Acute alcohol abuse
- Ciprofloxacin
- Ketoconazole (and other -azoles)
- Sulfonamides
- Quinidine
Sulfa Drugs (9)
Sulfa Allergy Pres (5)?
- “Popular FACTSSS” *
- Probenacid
- Furosemide
- Acetazolamide
- Celecoxib
- Thiazides
- Sulfonamide antibiotics
- Sulfasalazine
- Sulfonylureas
- Dapsone (for Leprosy)
PRES:
- Cytopenia
- Fever
- Hives / Pruritic rash
- Stevens-Johnson Sx
- UTIs
Nitro + Sulfa Drugs
Mech of Action, Mech of Toxicity (2)?
MECH: Oxidizing agents
TOX (MECH):
- Production of Methemoglobin
- Production of Hemolysis in G6PD Deficiency
↑in peroxide destroys RBCs
Electron Transport Inhibitors (4)
Mech?
MECH: Inhib e transport ->↓proton gradient.
- CO
- Cyanide
- Antimycin A
- Rotenone
ATP Synthase Inhibitor
Mech?
MECH: Inhib ATP Synthase -> Inhib e transport ->↑proton gradient.
- Oligomycin
Uncoupling Agents (3)
Mech, Pres (2)?
MECH:↑memb permeability -> ↓proton gradient.
- E transport continues
- ↑O2 consumption = Heat production + Hypoxia
PRES:
- Hypoxia
- Hyperthermia
- Alcohol
- Aspirin
- 2,4- Dinitrophenol (used illicitly for weight loss)
Erythema Multiforme -> Stevens-Johnson Sx ->
Toxic Epidermal Necrolysis
Causative Drugs (8: 2 Antibiotic Classes, 5 Epilepsy, 1 Gout)?
- Penicillins
- Sulfa Drugs
- Phenobarbital
- Phenytoin
- Carbamazepine
- Ethosuximide
- Lamotrigine
- Allopurinol
Arthus Rx
Mech, Pres (2)?
MECH: Type 3 HS- antigen-ab complexes form in skin.
PRES: After intradermal injection of antigen (eg Tetanus vaccine)
- Infl / Edema
- Necrosis
Jarisch-Herxheimer Rx
Mech, Pres?
MECH = Killed bacteria releasing pyrogens / toxins.
PRES = Flu-like sx after antibiotics (usually for Syphilis) started
Restrictive Lung Disease
Causative Drugs (4)?
- Amiodarone
- Bleomycin
- Busulfan
- Methotrexate
Reactions to Transfusion
- DIC
Disulfiram-like Effects
Def’n, Mech (3 steps), Causative Drugs / Drug Classes (3)?
(Antabuse). Hypotension, flushing + sweating, severe headache, nausea + vomiting.
MECH:
Inhib of Aldehyde dehydrogenase ->
Alcohol can’t be metabolized ->
↑in Aldehyde.
DRUGS:
- 1st Generation Sulfonylureas
- Cephalosporins
- Metronidazole
Lead Poisoning
Sign?
‘Burton Line’: Bluish line on gingiva
a-amanitin (in Amanita phalloides = “Death Cap mushrooms”)
Mech, Toxicity?
MECH = Inhib of RNA Polymerase II
TOX = Severe Hepatotoxicity
Arsenic Toxicity
Mech, Pres (3)?
MECH = Inhib of Lipoic acid (cofactor in Pyruvate Dehydrogenase complex).
PRES:
- Garlic breath
- Vomiting
- Rice-Water stools
Arsenic Exposure
Comp?
COMP:
- Squamous Cell Carcinoma
Drugs Contraindicated in Pregnancy
- Antibiotics (10: 6 antibiotics + 1 antifungal + 3 antivirals)
- Thyroid Drug
- Cancer Drug (Antimetabolite)
- CV / Renal Drug Class
- Sulfonamides -> Kernicterus
- Fluoroquinolones (-floxacin / oxacin) -> cartilage damage
- Aminoglycosides (-mycin) + Tetracyclines (-cycline)
- Macrolides (-thromycin)
- Chloramphenicol -> Gray Baby Sx
- Metronidazole -> Mutagenesis
- Griseofulvin
- Ribavirin
- Delavirdine + Efavirenz
- Methimazole
- MTX
- ACE Inhibitors
