Pharma Topic List A Flashcards
A.5. Local anesthetics Drugs
cocaine
lidocaine
articaine
bupivacaine
A.5 Local Anesthetics - MoA
blocks Na+ channel inhibiting AP
LA cause vasodilation add vasoconstrictor like E
Frequency dependent Blockade - affects depolarized nerves - sensory, A-delta, C - more than motor
Onset - LA with lower pKa have a quicker onset - since more drug will exist in unionized form. thereby it allows penetration into the neuron easier
A.5 Local Anesthetics - Factors Affecting half life of LA
- severe liver disease
- competition with other drugs fro the same enzyme
- decrease in hepatic blood flow
cocaine
Ester - metabolized by pseudocholinesterase
Topical
ISA - reuptake inhibiotr
DoA=1-2h
SE: - allergy, CV and CNS disturbance, coronary spasm, euphoria
A.5. Local anesthetics Drugs
lidocaine
amide - met CYP450 (CYP3A4)
Fast onset of action - short, local procedures
post-op analgesic
DoA - medium
can produce autonomic block in ischemic conditions - Class Ib antiarrythmic
Lidocaine interacts with antiepileptics
A.5. Local anesthetics Drugs
articaine
Amide
most rapid onset of action
very high potency
has an ester on its side chain - can be inactivated by hydrolysis
A.5. Local anesthetics Drugs
bupivacaine
Amide - CYP450 (CYP3A4)
Long duration of action
highest potency
high protein binding
used for long procedures
Cardiotoxic - severe myocardial depression esp if administered into blood
A.5. Local anesthetics Drugs
A.6. Glucocorticoids for oral and parenteral use - GC summary
GC-R are found through-out the body.
When they bind the GC-R complex dimerizes –> recruits coactivators or corepressors –> translocates into the nucleus, where it attaches to the GC-R gene element (GRE) –> gene expression modulation
Activation:
-Annexin1 –> dec PLA2
- enzymes for gluconeogenesis and AA metabolism
- adrenergic-R on vascular and bronchial smooth muscle
Repression:
COX2, NOS, cytokines, interleukins, cell adhesion molecules
A.6. Glucocorticoids for oral and parenteral use -Drugs
hydrocortizone
prednisolone
methylprednisolone
dexamethasone
triamcinolone
hydrocortizone
synthetic cortisol
short acting 8-12 hours
same affinity GC:MC
PO,IM, intra-art
Tx- DoC primary adrenocortical insufficiency (Addisons) or CAH - congenital adrenal hyperplasia
helps with IBD - enema
inibits peripheral conversion T4 to T3 - tx - thyroid storm
A.6. Glucocorticoids for oral and parenteral use
prednisolone
Active metabolite of prednisone
systemic steroid
PO, topical
intermediate acting 12-36 hr
GC:MC - 4 : 0.8
Tx - DoC for systemic anti-inflamm and immunosupression
inhibits cytokine gene expression
severe persistent asthma
thyrotoxicosis
A.6. Glucocorticoids for oral and parenteral use
methylprednisolone
Dose: 4 - 250mg
PO, parenteral
intermediate acting 12-36 hr
GC:MC - 5 : 0
TX - DoC for systemic anti-inflamm and immunosupression
thyrotoxicosis
IBD - PO or inj
Antiemetic in CIV
Urgent cases IV - anaphylaxis, bronchial asthma, brain edema, hepatic coma
A.6. Glucocorticoids for oral and parenteral use
dexamethasone
synthetic GC - Dexathemasone suppression test - suppresses cortical release in normal individuals but not in those with cushings
long acting 36 - 72 hours
DoC - supression of ACTH, anti-inflamm and immunosupress where water retention is unwanted
-IM mother within 48 hr premature birth to hasten fetal lung maturation
Neoplastic - dec brain edema
used in conjuction with aminogluthetimide to dec estrogen in breast cancer
A.6. Glucocorticoids for oral and parenteral use
triamcinolone
PO, Topical, parenteral
intermediate acting 12-36 hr
GC:MC - 5 : 0
Tx - allergic rhinitis spray
More Toxic than others
A.7. Mineralocorticoids. Topically applied glucocorticoids Drugs
fludrocortizone
fluocinolon
mometazone
budesonide
fluticazone
metyrapone
A.7. Mineralocorticoids. Topically applied glucocorticoids Drugs - Effect of MC
MC are steroids produced by the adrenal cortex. MC-R complex effects gene expression.
Genomic Receptor Action:
- inc Na+/K+ transcription
- inc ENaC channel activity
- inc expression of pro-fibrotic molecules
- inc NADPH expression
- inc ROS pro-inflam
Non-Genomic
- inc Na+ reabsorption
- inc K+ and H+ excretion - via collecting duct
fludrocortizone
MC
DoC for replacement therapy for adrenal hypofn
Acute/Chronic or post Adrenalectomy
PO
long duration of action
inc Na+ reabsorption in distal tubules and K+ ad H+ efflux
A.7. Mineralocorticoids. Topically applied glucocorticoids
fluocinolone
MC
TX - implanted in chronic non-infectious uveitis
ointment in derma
A.7. Mineralocorticoids. Topically applied glucocorticoids
mometazone
Topical GC - Aerosol - bronchial asthma
nasal spray - allergic rhinitis
A.7. Mineralocorticoids. Topically applied glucocorticoids
budesonide
Topical GC Aerosol - bronchial asthma
Nasal Spray - allergic rhinitis
Enema in IBD (suppository)
A.7. Mineralocorticoids. Topically applied glucocorticoids
fluticazone
Topical GC - aerosol in bronchial asthma
A.7. Mineralocorticoids. Topically applied glucocorticoids
metyrapone
Adrenocortical antagonist
inhibits beta hydroxylase - in ACTH producing tumors
used to dx test of ACTH fn
can be used to tx Cushings
A.7. Mineralocorticoids. Topically applied glucocorticoids
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity - Drugs
testosteron-undecanoate
bicalutamide
finasteride
goserelin
degarelix
sildenafil
nandrolon
testosteron-undecanoate
Synthetic steroid.
NOT PO – high first pass metabolism – transdermal patch, inject, gel.
TX- replacement tx in hypogonadism, maintain libido.
In case of PO needs to be absorbed with lipophilic vehicle into lymphatics.
SE – enhance hematocrit, excessive masculinization.
CI – prostate or breast cc. interact – may improve glucose tolerance, enhance anti-coagul in coumarins.
A.8. Androgens, anabolic steroids, antiandrogens. Agents affecting the sexual activity