Pharmaco 💊 Flashcards
P450 INDUCERS
CRAPGPS
Carbamazepine
Rifampin
Alcohol
Phenytoin
Griseoflavin
Sulfonylurea
MOA of P450 inducer
Speed up drug metabolism
i.e, Increase clearance
P450 subtypes
CYP 1A2/2E1/2C9/2D6/3A4
Acetaminophen
Ethanol
Warfarin (K dependent - 2/7/9/10)
CVS drugs ( ECHO-2D)
Most common most drugs /toxin
Pharmacodynamic means
Conc of drug and it effect
How the drug interact with the body
Eg: Receptor+Ligands complex
Pharmakinetics stages
Absorption
Distribution
Metabolism
Excretion
Bioavailability
Amount of drug available in the systemic circulation ( blood)
IV- 100% available
PO- < 100% due to barriers( BBB/ Placenta/ GI tract /Testicular)
Potency of drugs
Strength of drug depending on dosage
Efficacy
Maximum effect independent of the dose ( max response drug can give)
Affinity of drugs
Ability of drug ligand to bind to receptors
Affinity & Potency(I.e: the more affinity the more molecule of drug bind to receptor and not leaving out unbound wasted drug molecules)
Antibiotic classes
- Cell wall inhibitor/B-lactamase - penicillin / Amoxicillin
- Protein synthesis inhibitor
-50s Ribosomal - tetracycline /aminoglycoside
-30s ribosomal - macrolide /clindamycin/linezolid/chlorenphenicol
3.NA inhibitor
- DNA gyrase ( Quinolones)
-RNA Pol(Rifampin)
4.Folate synthesis inhibitor (SMP-TMX)
Most common Empirical Antibiotics
1.Piperacillin + Clavulanate (or) tazobactem
-covers all except MRSA and Atypical
- 5th Gen cephalosporin (cover all except Pseudomonas and Atypical )
Antibiotics against Pseudomonas
3rd and 4th gen cephalosporin
Piperacillin+ clavulanic acid (or) Tazobectam
Quinolones
Aminoglycosides
Fosfomycin
Colistin
Antibiotics against MRSA
5th gen Cephalosporin
Folate antagonist (SMX-TMP)
macrolides/Clindamycin/Vancomycin/Linezolid (NA-I)
Tetracycline (30s)
MOA of Acyclovir
Treat what viral illness ?
Inhibit DNA polymerase by mutating viral thymidine kinase
Adding 3 phosphate chain to acyclovir which interfere with DNA replication
HSV/VZV
MOA of Oseltamivir
Used to treat which viral illness?
What other drugs can be used and MOA?
Influenza
1.Oseltamivir- Prevent release of copied virus into plasma via blocking viral attachment to cell membrane
2.endonuclease Inhibitor ( mRNA for viral translation and replication)
3.M2 Ion channel inhibitor ( block Viral genome released to host nucleus)
HRT of HIV MOA
- Entry inhibitor ( CD4 Receptor -I / C5R/CXCR -4-I)
- Reverse Transcriptase Inhibitor ( NRTIS/NNRTIS)
- Integrate Inhibitor
4.Protease inhibitor (prevent viral protein cleavage»_space; viral protein loss virulence)
ART regime in HIV
Most preferred / 1st line
1. 2NRTIS + NNRTIS
AZT + 3TC+EFV (zedovudine+Lemivudine + Efavirenz)
- 2 NRTIS + PI
Volume Distribution equation
Vd = Amount of Drug / Conc of plasma
Therapeutic Index (TI)
Is high TI good?
TI - minimum amount of drug to be effective
High TI is bad bc it means drugs needed a lot to be effective which can leads to toxicity and ADR
Half life equation
HL(t1/2)= 0.7 x Vd/CL(clearance )
How many half life needed for the drug to be eliminated or metabolized completely ?
Between 4 and 5 half life
Half life happen via 1st order elimination -happen to most drugs
Drugs with 0 order elimination
Ethanol
Aspirin
Phenytoin
Types of G Protein Receptor
- Gs- increase cAMP ( all b, H2 D2 receptors)
2.Gi - decrease cAMP (MAD2)
3.Gq - PIP /IP3 (M1 /M3)
Adrenergic receptors ( Sympathetic)
Alpha 1 (NE>E)-vasoconstriction /bronchoconstriction
Alpha 2 (E>NE)- inhibit Glu,cAMP,Insulin,NE
Beta1 (E=NE)- Increase HR/Lipolysis / heart contraction , Renin
Beta 2 (E>NE)- vasodilation /Bronchodilation/glycogenolysis
Cholinergic receptors
Muscurinic -M1 to M5 - Act on NMJ
Nicotinic - Nm/Nn (ligand gated R)- act on CNS/adrenal glands )
Nitric Oxide and cGMP signaling
Vasodilation
Muscle Relaxation
NO acts on cGMP and cause dephosphorylation of myosin light chain along with endogenous compound (Bradykinin / His)
