PASS/FA Pharm Drill Day 3

a. < 1 half-life
b. 3.3 half-lifes"

T1/2 = (Vd/Cl) x .7

MD = (Css x Cl) / f

All drugs except:
*EPA
Ethanol
Phenytoin
Asparin (high dose)

Phase II

*TILE
TI = LD50 / ED50

"It doesn't: efficacy (Vmax) is not affected
However, potency is decreased (Km is increased) and therefore the POTENCY curve is shifted to the right

"It doesn't: potency (Km) is not affected (the drug is just as potent as before, but some receptors are turned off)
However, efficacy (Vmax) is decreased and therefore the EFFICACY curve is shifted downward

"*CCELLS (Buys AT 30 CCELLS at 50)
Chloramphenicol
Clindamycin
Erythromycin
Lincomycin
linezolid
Streptogramins

"Sulfonamides
Trimethoprim
Methotrexate
pyrimethamine

Quinolones

"*HEN PEcKS (c = cocci)
H. Influenza
Enterobacter
Neisseria
Proteus
E. Coli
Klebsiella
Serratia
G+ cocci

Ceftazidime

Enterobacter

"Pt's who cannot tolerate AMG's
OR
Pt's who are allergic to Penicillin
OR
Pt's in Renal Failure

Any G- rod

"*VACUuM THe BR
Vibrio
Acne (Propionibacterium Acnes)
Chlamydia
Ureaplasm Urealytica
Mycoplasm
Tularemia
H. Pylori
Borellia
Rickettsia

"*UPS Lost My Brand New Car
URI's (caused by G+ cocci)
Pneumonia (caused by G+ cocci)
STD's (caused by G+ cocci)
Legionella
Mycoplasma
Bordatella
Neisseria
Chlamydia

Bacterial Meningitis

Anaerobes above the diaphram

Inhibits initiation complex at 30S causing misreading of mRNA

Inhibition of tRNA charging by preventing attachement of amino acyl tRNA

Blocks ADH receptors

*AzTHREEonam
Binds to PBP #3

"Inhibits Peptidyltransferase, the enzyme responsible for transferring nucleotides from A --> P site

Inhibits peptide bond formation

"Griseofulvin
Flucytosine

"*CAT
Caspofungin
""Azoles""
Terbinafine

Amphotericin B
Nystatin

"Systemic fungal infections
Severe sepsis (103 F)

"Systemic fungal infections that are neither severe nor septic
All topical fungal infections

"Oral Candidiasis
Topical

Changes uracil to fluro-uracil

Any systemic fungal infection

Inhibits Theta-13 Delta-Glucan

"*CASPofungin
ASPergillosis (invasive)
Systemic Candidiasis

Inhibits cell wall synthesis by blocking squaline epoxidase

"Dermatophytes
Superficial fungal infections

Griseofulvin

Binds microtubules, arresting the cell in mitosis

Severe &/or septic SYSTEMIC fungal infections:
--Amphotericin B
SYSTEMIC fungal infections:
--Azoles
--Flucytosine
--Caspofungin
TOPICAL fungal infections:
--Azoles
--Nystatin
--Terbinafine
--Griseofulvin

"Prevents viral ""uncoating""
Prevents viral penetration
Increases DA

"*Influenza A, RubellA & the CerebellA
Influenza A
RubellA
Parkinson's (the CerebellA)

Oseltamivir
Zanamivir

Inhibits viral influenza neuraminidase, decreasing the release of viral progeny

"Acetaminophen

Full Name: N-Acetyl-Para-Aminophenol (APAP)
Other Names: Tylenol (U.S.)
Paracetamol (outside North America)

"Inhibits Guanine nucleotide synthesis by competitively inhibiting IMP Dehydrogenase
"

"Chronic Hepatitis C
RSV

"Ribavirin
INF-alpha"

INF-alpha
Lamuvidine

Lamivudine or 3CT is an NRTI

Lactic Acidosis

MS

CGD (NADPH oxidase deficiency)

"INF-alpha: Hep B & Hep C (""ABC"" --> aBC or alpha B C)

"Inhibition of viral DNA polymerase when phosporylated by the VIRAL thymidine kinase

Any HSV except HSV III and HSV V

HSV I = Oral herpes
HSV II = Genital herpes
HSV III = VZV
HSV IV = EBV
HSV V = CMV
HSV VI = Roseola
HSV VII = Pyteriasis Rosie
HSV VIII = Kaposi's Sarcoma

HSV III = VZV
Chicken Pox Tx = Valcyclovir
Herpes Zoster Tx = Famciclovir

HSV V = CMV
Tx with Ganciclovir or Foscarnet

"Inhibits CMV viral DNA polymerase when phosphorylated by VIRAL thymidine kinase

Binds to pyrophosphate binding site;
Does NOT REQUIRE phosphorylation by VIRAL thymidine kinase

Ganciclovir followed by Foscarnet

*SIR AN (NAVIR tease a protease)
Saquinavir
Indinavir
Rotinavir
Amprenavir
Nelfinavir

Inhibition of aspartate protease

Crystal-induced Nephropathy
Thrombocytopenia

*Nevada/Deleware/E-Fuck Virus or NEVIR Efir (ever) DELiver nucleosides
Nevirapine
Delavirdine
Efavirenz

SJS

SJS
Hepatotoxicity

AZT/ZDV --> Ziduvidine
DDI --> Didanosine
DDC --> Zalcytobine
3TC --> Lamuvidine
D4T --> Stavudine
ABC --> Abacavir

All NRTI's: Lactic acidosis

Ziduvidine (AZT/ZDV)
--Aplastic anemia
--Megaloblastic anemia
Didanosine (DDI)
--Drug-induced pancreatitis
Zalcytobine (DDC):
--SJS
--Peripheral neuropathy
Lamuvidine (3TC)
--only lactic acidosis
Stavudine (D4T)
--Peripheral neuropathy
Abacavir (ABC)
--Hypersensitivity syndrome

Binds to GP41 & prevents VIRAL & CELLULAR membrane fusion

Suramin

Nifurtimox

1st: TMP/SMX
2nd: Aerosolized Pentamidine
3rd: Dapsone

NOTE: PCP = PneumoCystis Pneumonia
BUG: Pneumocystis Jiroveci (formerly Pneumocystis Carinii)

Drug-induced pancreatitis

Metronidazole

*GET GAP
Giardia
Entamoeba
Trichamona
Gardnerella
Anaerobes
H. Pylori

Primaquine for "latent" hypnozytes (otherwise tx = Chloroquine)

Methloquine
Malaria from the indian subcontinent/subsahara is assumed to be resistent to Chloraquine

"Chloroquine tx's Malaria
Primaquine tx's ""Latent"" Hypnozites (P. Vivax/P. Ovale)
Methloquine tx's Resistent Malaria (Indian Subcontinent/Subsahara)

Pentavir Antimony
Na+ Stipigluconate

Niclosamide
Note: WIKI says Praziquental (1st) or Niclosamide (2nd)

B12

Vitamin C

Praziquental (h/w on day 11 shazhad says

Pyrantal Pamoate followed by Mebendazole

Mebendazole/Albendazole

Ivermectin

Vesimicol

Hemicholinium

Botulinum Toxin

Reserpine

Guanethidine

Amphetamine

Cocaine
TCA's

Angiotensin II

M1 & a2

Methanacol
Bethanacol
Carbichol
Pilocarpine

Neostigmine
Pyridostigmine
Physostigmine
Edrophonium
Echothiophate

Added Day 10:
Rivastigmine
Galantamine
Tacrine (partial muscarinic agonist)
Donepezil

Physostigmine
Echothiophate

Edrophonium

Tensilon test

Physostigmine

Neostigmine
Pyridostigmine

Neostigmine

Bethanachol

Asthma Challenge Test

The same as indirect cholinomimetics (AChE Inhibitor means ""indirect""):
Neostigmine
Pyridostigmine
Physostigmine
Edrophonium
Echothiophate

*My Grandma Don't Remember Things
Memantine**
Galantine
Donepazil
Rivastigmine
Tacrine

**Memantine is NOT an AChE Inhibitor; its MOA is to block NMDA Glutamate receptors, 5-HT & D2 receptors, and nicotinic ACh receptors

*ADDUMBBELSS
Abdominal cramping
Diaphoresis
Diarrhea
Urination
Miosis
Bradycardia
Bronchospasm
Excitation of skeletal muscle
Lacrimation
Secretion
Salvation

"Sweating is a SS response (activated by sympathetics) under PS control (ACh is the NT); this is why sweating is affected by drugs that affect ACh levels &/or ACh rec's, even though it is a SS response.

Atropine followed by...
Pralidoxime (2-PAM)

Blocks SLUD (anti-PS):
Salivation
Lacrimation
Urination
Defication

*Hot as a Hare: Warm skin (dec'd sweat --> reflex vasodilation)
Dry as a Bone: Dry skin/eyes (dec'd sweat/dec'd lacrimation)
Red as a Beet: Flushing (reflex vasodilation secondary to dec'd sweat)
Blind as a Bat: Mydriasis/Cycloplegia (dec'd PS's)
Mad as a Hatter: Confusion/Disorientation (CNS effects on M4/M5 rec's)

NOTE: Decr'd sweating (SS response under PS control) --> incr'd body temp --> compensatory cutaneous vasodilatory response ==> REFLEX VASODILATION

Atropine

Pacemaker

Nicotinic ACh receptor antagonist

Ganglionic blocker (muscle relaxant)

"*2nd-rate alpha-male MD
a2, M2, D2 --> Gi --> decr'd AC = decr'd PKA = decr'd cAMP =
decr'd SS outflow & incr'd PS outflow

Story: An ""alpha""-male"" got an MD from a 2nd-rate Carribean school. Having come from a 2nd-rate school, he is very negative (inhibitory or Gi)

*1st-rate alpha-male MBA who has plenty of $
a1, M3, H1, M1, V1 --> Gq --> Incr'd PLC = Incr'd PKC = Incr'd IP3/DAG =
Incr'd calcium release

Story: An ""alpha""-male"" got an MBA from a 1st-rate American school. Having come from a 1st-rate school, he has lots of $$$. He drives an M3 and a HuM V. He also wears really nice clothes featured in Gq magazine.

"*Any receptor not included in Gi or Gq is defaulted to Gs, where s = stimulatory
B1, B2, D1, H2, V2 --> Gs --> Incr'd AC = Incr'd PKA = Incr'd cAMP =
Incr'd SS outflow & Decr'd PS outflow
"

Heart & Kidney: B1 & M2
Vessels & Sphincters: a1 & M3
Other Organ Systems: B2 & M3

1. a1/B1 --> Contraction/Incr'd Fxn
2. a2/B2/M2 --> Relaxation/Decr'd Fxn
3. M3 Muscles/Glands/Pancrease --> Contraction/Incr'd Fxn
4. M3 Sphincters --> Relaxation/Decr'd Fxn

a2, M2, & D2 --> Gi --> Decr'd cAMP --> Decr'd SS outflow & Incr'd PS ouflow

a1, M3, H1, M1, V1 --> Gq --> IP3/DAG --> Incr'd calcium release

Gq

IP3/DAG

a1 --> Gq --> IP3/DAG --> Incr'd calcium release -> muscle contraction = VC

a2 --> Gi --> Decr'd cAMP --> Decr'd SS outflow & Incr'd PS ouflow

a2 --> Gi --> Decr'd cAMP --> Decr'd insulin release (i.e. decr'd function)

B1 --> Gs --> Incr'd cAMP --> Incr'd SS outflow & Decr'd PS ouflow

B2 --> Gi --> Decr'd cAMP --> Decr'd HR, decr'd contractility, decr'd conduction (i.e. decr'd function)

B2 --> Gi --> Decr'd cAMP --> Decr'd insulin release (i.e. decr'd function)

B2 --> Gi --> Decr'd cAMP --> Decr'd lipolysis (i.e. decr'd function)

B2 --> Gi --> Decr'd cAMP --> Decr'd tumor formation (i.e. decr'd function)