Drugs 4 Albin

Section

Question	Answer
Daptomycin	Rapid depolarization of cell membrane → disruption of DNA,RNA synthesis → cell death.
Daptomycin Dx	Vancomycin Resistant, MRStaph Aureus, Cornybacteria
Daptomycin Sx	Diarrhea, Nausea, Rhabdomyolysis
Trimethoprin	Inhibits bacterial dihydrofolate reductase(pyrimidine synthesis)- converting dihydrofolic - tetrahydrfolic
Trimethoprin Dx	TMP-SMX → UTI, Shigella, Salmonella, Pneumocystis Jirovecii(<200 Aids Prophylaxis)
Trimethoprin Sx	MegaloblasticAnemia, Steven Johnson Syndrome, Toxic epidermal necrolysis, Leukopenia, Granulocytopenia, Sulfa Allergy
Rifampin	Inhibits DNA dependant RNA polymerase. Rapid resistance if used by itself(Altered structure of bacterial ribosomal proteins).
Rifampin Dx	Mycobacterium TB, Leprosy, Meningococcal Prophylaxis(MONOTHERAPY).
Rifampin Sx	Red orange or orange body fluids, Hepatotoxic.
Isoniazid	Decrease synthesis of Mycolic acids. Mutation causes resistance becauses KatG(BACTERIAL Catalase peroxidase) needed to activate isoniazid. 2. Modification of the protein target binding site.
Isoniazid Dx	Mycobacterium TB and Prophylaxis of TB
Isoniazid Sx	Neurotoxicity can be prevented by giving b6, SLE, Hepatits(Hepatocyte damage) G6PD, Seizures
Isoniazid Antidote	Pyridoxine
Pyrazinamide	Pyrazinamidase → pyrazinoic acid. (Requires and Acidic Environment to kill TB inside the phagosome of macrophages and other intracellular organisms)
Ethambutol	Ethambutol-arab-carbohydrate Blocks Arabinosyltransferase → Decreases Carbohydrate polymerazation of cell wall. Mutation causes resistance Increases acitivty of enzymes involved in cell wall polysaccharide synthesis.
Ethambutol Sx	Optic Neuropathy/ Red green color blindness.
Streptomycin	TB drug. Resistance caused due to altered structure of bacterial ribosomal protein
Streptomycin	Inhibits initiation of protein synthesis by binding to and distorting the structure of prokaryotic 30 s ribosomal subunit
	memorize

 

: Antifungal

Question	Answer
Amphotericin B	Binds ergosterol and forms leaky membrane pores TOPICAL
Amphotericin B Dx	Cyptococcus, Blastomyces, Coccidioides, Histoplasma, Candida, Mucormycosis.
Amphotericin B Sx	Renal Toxicity, Optic Neuropathy, Redgreen color blindness
Amphotericin B Major Sx	Serum potassium and magnesium needs to be monitored.
Flucytosine	Fluctysoine converted to 5-FU in fungal cells → Inhibits DNA and RNA synthesis.
Flucytosine Dx	Cryptococcal Meningitis with Ampotericin b
Nystatin	Binds ergosterol and forms leaky membrane pores TOPICAL
Nystatin Dx	Candidiasis, topical- Diaper rash, Vaginal Candidiasis.
Azoles	Inhibit 14α-demethylase, a cytochrome P450 enzyme required for ergosterol synthesis.
Azoles Dx	Cryptococcal Meningitis in AIDS, Blastomyces, Coccidioides, Histoplasma, Candida.
Azoles Sx	Inhibiton of testosterone synthesis → Gynocomastia. Liver dysfunction → Inhibit P450.
Terbinafine	Inhibits Fungal Squalene Epoxidase → Ergosterol Synthesis Inhibited
Terbinafine Dx	Dermatophyte infections TOPICAL
Terbinafine Sx	Abnormal Liver function tests & Visual Disturbances
Griseofulvin	Binds to microtubules → Disrupts mitotic spindles.
Griseofulvin Dx	Superficial infections, Dermatophyte infections TOPICAL
Griseofulvin Sx	Carcinogenic, Teratogenic, Confusion, headache, Induce p450
	memorize

 

: Anti-protozoan

Question	Answer
Chloroquine	Blocks detoxification of Heme → Heme accumulates
chloroquine Dx	Plasmodial infections except P.falciparum
Chloroquine Sx	Retinopathy
Pyrimethamine and Sulfadiazine	Toxoplasma gondii – HIV – Ring or spherical frontal lobe calcifications MRI
Primaquine ALWAYS+ WITH chloroquine	FOR P.Vivax & P.Ovale = Prevent Disease relapse due to intrahepatic stages.
Mebendazole	Enterobiasis FIRST-LINE
Mefloquine	First line for Plasmodium
	memorize

 

: Viral

Question	Answer
ZanaMiViR, OseltaMiViR	Inhibit Influenza neuraminidase → decreased Membrane Viral Release (Lysogeny), viron particle release
ZanaMiViR, OseltaMiViRDx	Influenza A&B = Prevention and treatment
ZanaMiViR, OseltaMiViRSx	Retinopathy
Ribavirin	Competivily inhibit IMP Dehydrogenase → Inhibit synthesis of guanine Nucleotides → interfere with duplication Viral genetic material
Ribavirin Dx	RSV, Chronic Hepatitis C
Ribavirin Sx	Hemolytic Anemia, Extremely Teratogenic
Amantidine	Impairs uncoating or disassembly of influenza
Acyclovir	Purine nucleoside analogue → Viral thymidine kinase converts it into acyclo-GTP → Inhibits Viral DNA Polymerase & incorporation into viral DNA → chain termination.
Acyclovir Dx	HSV & VZV
Acyclovir Sx	Renal tube crystalline nephropathy – Adequate Hydration must be given
Valacyclovir	Given daily to prevent recurrence of HSV-2
FosCARnet	Pyrophosphate analogue that inhibits viral DNA polymerase by binding to pyrophosphate binding site of enzyme. No viral kinase required. Also inhibits NRTI
FosCARnet Dx	Used in acyclovir/ganiciclovir-Resistant hsv, Cmv retinitis, advanced Aids
FosCARnet Sx	Nephrotoxicity → Hypocalcemia, Hypomagnesemia,Hypokalemia → Seizures
Zidovudine	Used for general prophylaxis and during pregnancy to reduce transmission risk. Decrease vertical transmiZion. Sx Blasts your bonemarrow, Megaloblastic anemia
Enfuvirtide	Bind HIV gp-41 protein leading to preventing gp41 from allowing virus to fuse to target cellullar membrane
NNRTI	Bind to reverse transcriptase at a different site. Do not need a thymidine kinase to be activated. Does not need activation via intracellular phosphorylation.
NNRTI Sx	Bone Marrow Suppression(G-csf), Peripheral Neuropathy, Lactic Acidosis(nucleosides), Rash(non-nucleosides), Megaloblastic anemia(ZDV)
NNRTI drugs	NeVIRapine, EfaVIRenz, DelaVIRDINE
ProTEASE Inhibitors – “navirs”	Inhibit viral in coded protease to cleave polyproteins → Prevent maturation
ProTEASE Inhibitors – “navirs Sx	Hyperglycemia, GI intolerance, Lipodystrophy (FAT REDISTRUBITION - Cushing)
ProTEASE Inhibitors – “navirs	LopiNAVIR, AtzaNAVIR, FozampreNAVIR,SaquiNAVIR
Integrase Inhibitor	Inhibits HIV viral genome integration into host cell chromosome by reversibly inhibting HIV integrase → Impairs Messenger RNA Transcription
RalTEGRAvir Integrase Inhibitor Sx	Hypercholesterolemia
Integrase Inhibitor Drug	RalTEGRAvir
	memorize

 

: Antidotes

Question	Answer
Mushrooms	Death cap – Aamanitin → inhibits RNA polymerase II “MRNA” → liver fail
Acetaminophen	Inhibit COX enzyme → Inhibiting pro-inflammatory chemicals. Metabolized by AM404 → Reuptake of Anandamide by neurons/ Inhibit Na Channel(Anesthetic) Normal – Conjugated by liver → N-acetylbenzoiminoquinone → Glutahione molecules reacts → Urine
Acetamenophen Abnormal	Liver → ↑N-acetylbenzoiminoquinone → ↓Glutahione molecules → Zone III Centriolobular Hepatic necrosis.
Acetamenophen Antidote	N-acetylcysteine → glutahione precursor → ↑ Glutahione molecules for NAPQI
N-acetylcysteine	Also used in Cystic Fibrosis pts as mucolytic agent by cleaving or reducing the intermolecular disulfide bridges or bonds within mucus glycoproteins
N-acetylcysteine non toxic	Sulfhydryl group supplementation for acetaminophen toxicity
↑Iron - Hemachromatosis Sx	CNS, Bloody Diarrhea, Metabolic acidosis, Restrictive cardiopathy, joint pain, diabetes, skin bronze
↑IronAntidote	Deferoxamine
Lead Sx	Microcytic anemia, abdominal pain, purple lines on gingivia, Peripheral Neuropathy.
Lead Antidote	Edta, Dimercaprol
Methemoglobin “Chocolate apperance Blood”	Sx Cyanosis, Fatigue, Confusion, Coma
MethemoglobinAntidote	Methylene Blue
Arsenic	Garlic smelling breath, CNS, Mees Lines(white horizontal lines on fingernails
Copper – Skin yellow, Wilsons liver disease(low ceruloplasmin)	Penicillamine
Mercury – Fish, fluorescent light bulb	Dimercarpol
Prinzmitel Angina	Elevated ST segment with lead changes
Ergonovine	Used to test for prinzmitel Angina
CyanideSx	Almond scent breath, trismus, apnea, seizures, coma, cardia arrest.
CyanideTx	Amynitrate – Convert to Methhemoglobin - > ferrous iron means cyanide binds more to ferrous iron and NOT mitochondrial enzymes = LESS DAMAGE
Nitropusside poisioning	↑Cyanide → Metabolic Acidosis → ↑Venous po2 = REVERSE WITH SULFUR which increases-> Sodium thiosulfate coverts it to Thiocyanate → excreted
Bromodeoxyuridine (Thymidine)	Increase uptake means high number of tumor cells in s phase waiting to replicate and signifies High grade
	memorize

Sideeffect

Question	Answer	Column 3
Statins	Treat High Ldl	Hepatits, Myopathy
Niacin	Treat low HdL	Cutaneous Vasodilation, Hyperuricemia(gout), Hyperglycemia(Acanthosis nigracians), Hepatits
Fibrates	Treat High Triglyceride	Gallstones, Myopathy(worse with statins)
Bile acid resins	Treat High LdL	GI Upset, Hypertriglyeridemia, Malabsorption
		memorize

MRSA Infection drugs

Question	Answer
Vancomycin	blocks glycopeptide polymerization by binding tightly to d-ala-d-ala
Vancomycin	Redman Syndrome, Nephrotoxicity
DaptoMYCIN	Depolarization of cellular membrane
DaptoMYCIN	Myopathy and CPK elevation
DaptoMYCIN	Inactivated by pulmonary surfactant
linezolid	Binds to 50s and inhibits protein synthesis
Linezolid	Thrombocytopenia, Optic Neuritis, Risk for serotonin Syndrome
C.difficile	Metrondiazole, vancomycin, Fidaxomicin
Severe Cdifficile	Vancomycin
Recurrent Cdifficile	Fidaxomicin
Fidaxomicin	Oral drug with minimal systemic absorpotionand less affecton normal colon than vancomycin and metrondiazole
	memorize

Teratogenic

Question	Answer
Tetracyclines	Teeth Discoloration
Aspirin	Neonatal Bleeding
Cocaine	Fetal growth retardation
Alcohol	Fetal Alcohol Syndrome (Mental retardation, mid face abnormalities)
Diabetes	Caudal Regression Syndrome (sacrum and lumbar not developed leading to flaccid paralysis/absent ankle reflex)
Marijuana	Low birth weight babies
	memorize

Overdose

Question	Answer
Phencyclidine	Nystagmus, Violent behavior,ataxia
LSD	Visual Hallucinations
Coccaine	Chestpain, seizures
Methamphetamine	Toothdecay, Tachycardia, diaphoresis, violent behavior, choreiform movements
Marijuana	Increase Appetite, Impaired Time perception, Conjunctival injection
Heroin	Depressed mental status, Miosis, Respiratory depression
Alcohol withdrawal DOC	Diazapam & Chlordiazepoxide
	memorize

Benzodiazepines

Question	Answer
MOA	Allosteric binding to the gaba receptor and increasing the frequency of ion channel opening
Zolpidem	Least addictive sleeping aid
Triazolam	SHORT
Alprozalam	Short
Lorazepam	Intermediate
Diazepam	LONG
Flurazepam	LONG
Chlordiazepoxide	LONG
	memorize

 

: Antiandrogens

Question	Answer
Finasteride moa	5a reductase inhibitor → ↓testosterone to DHT → Decrease in ONLY DHT levels. Dx Baldness, B+PH
Finasteride Sx	Gyncomastia
Flutamide moa	Competitive Inhibitor of testosterone receptor and DHT → Dx prostate carcinoma
Ketoconazole moa	Inhibits 17,20 Desmolase → Dx In Poly Cystic Ovarian Disease Prevent Hirsuitism
Spirnolactone moa	Inhibits androgen receptor with its interaction with DHT
Spirnolactone Sx	Gyncomastia, Hair Loss
	memorize

 

: Dopaminergic

Question	Answer	Column 3
Mesolimbic - Mesocortical	Regulates Behavior	Schizophrenia
Nigrostriatal	Cordination of voluntary movements	Parkinsonism
Tuberoinfundibular	Controls Prolactin secretion	Hyperprolactinemia
		memorize

 

Beta blocker sideffect

Question	Answer	Column 3
Bronchic	Bronchoconstriction and can asthma or COPD worse	B2 Blocker
Muscle vasculature	Vasospasm Make peripheral artery disease worse	B2 blocker
Glucagon Secretion	Diminished in pts with DM	B2 Blocker
Heart ONLY	B1 Blocker	Decrease Sa & Av Node helpful in atrial arythemias
Heart Only	B1 blocker	Reduce O2 consumption leading to less angina in MI
Heart Only	B1 Blocker	Decrease HR & Contractility to lower BP
Insulin inhibited	A receptor	Stimulated
Insulin secreted	B & H2 receptor	Stimulated
		memorize