Pharmacology notes Topnotch Flashcards
Neural tube defect
Valproic acid
Fetal renal damage / renal agenesis
ACE inhibitors
Fatal hydantoin syndrome
Phenytoin
Neonatal hypoglycemia
Oral hypoglycemic agents
Vaginal clear cell Ca
DES
Eibstein anomaly
Lithium
Craniofacial malformations
Tetinoin
Congenital hypothyroidism
Iodide
Möbius sequence
Misoprostol
Cutis laxa
Penicillamine.
Used for Wilson’s ds
Phocomelia
Thalidomide
IUGR
Smoking
Ototoxicity
Streptomycin
Aplasia cutis congenita
Methimazole
Kernicterus
Sulfonamide
Cartilage damage
Foroquinolones
DNA gyrase/ topoisomerase II
Trial when careful evaluation of dose response relationship and pharmacokinetics among NORMAL human volunteers
Phase 1 trial
Evaluate drug in patients with target ds
Phase 2 trial
Trial involving many patients and clinicians
Phase 3 trial
Detects toxicities/ post marketing surveillance
Phase 4 trial
Inhibits transport of CHOLINE used in ACh synthesis
Hemicholin
Inhibits transport of ACh to vesicle for storage
Vesamicol
transport Vehicle inhibitor:)
Inhibit AChE in NMJ
Organophosphates
For bowel and bladder atony
Betanichol
- Cholinomimetic, direct, bind to muscarinic R
Used for SICCA syndrome of Sjorgen
Pilocarpine
- cholinomimetic.direct, bind to muscarinic R
- Increase aqueous humor flow and salivation.
Amanita phalloides MOS
RNA polymerase II inhibitor
S/sx organophosphate poisoning
nerve gas poisoning, cholinergic excess, inhibition of ACHe
Diarrhea
Urination
Miosis
Bronchospasm Bradycardia Excitation of Sk muscle and CNS Lacrimation Sweating Salivation
Bonds in order of strength
Covalent bond > ionic/hydrogen/van der waals bonds > hydrophobic bond
Indirect acting cholinomimetic ?
Bind AChE to prevent removal of ACh from ACh receptor
Edrophonium short acting
Longer acting
Neostigmine
Pyridostigmine
Physostigmine - glaucoma. Can cross BBB.
Cholinorecetor/muscarinic blockers
Anti muscarinic
1 M1 selective
2 non selective - atropine, scopolamine
Anti-nicotinic
1ganglion blockers
2 neuromuscular blockers - tubocurarine etc
Cholinesterase regenerators
1 pralidoxime
Other
Ipratropium
Muscarinic antagonists for PD
Trihexyphenidyl
Benztropine
Biperidine (akineton)
Atropine toxicity
Hot as a hare Dry as a bone - dec secretions Red as a beet - cutaneous vasodilation Blind as a bat - dilated pupils Mad as a hatter
Neuromuscular blockers
NDMB - non depolarizing
DMB - depolarizing
NDMB: Tubocurarine, pancuronium, atracurium, verocurium
DMB : succinylcholine
Kidney dopa vs NorE
Dopamine vasoDilates the afferent arterioles, while NorE vasoconstricts them
NorE transmitter at sympathetic post ganglionic except in
Eccrine sweat glands
Vasodilator sympathetic fibers in skeletal muscle
These use ACh acting on muscarinic receptors
Inhibits hydroxylation of tyrosine to DOPA
ie inhibits NorE synthesis
Metyrosine
Inhibits transport of NorE and Dopamine in vesicles for storage
ie inhibits storage
Reserpine
Monoamin oxidase inactivate NorE and dopamine in the cytoplasm
Effect of MAO inhibitors?
Increase store of NorE and Dopamine
Inhibits release of NorE
Guanethiadine
Promotes release of NorE 2
Amphetamines
Tyramine - found in cheese etc, relate to antidepressant MAO
inhibitors
Inhibit reuptake of NorE from receptor such that NorE action cannot be terminated
1 cocaine
2 TCAs
Inhibit degradation of NorE into metanephrine and VMA
MAO inhibitors, COMT inhibitors
Beta receptors b1 vs b2
1 heart, 2 lungs
B1 heart
B2 bronchodilation
Non selective sympathomimetics
1 Epi. Alpha1, B1, B2 2 NorE Alpha1, B1, B2 3 Dopamine 1 -5 mcg/kg/min low D1 vasodilate splanchnic and renal bed 5-15 medium B1 > 15 high alpha1
Non selective beta agonist
Isopreterenol
Alpha 1 agonist
Alpha 2 agonist
Alpha 1 agonist. Pseudoephedrine
Alpha 2 agonist. Clonedine, Methyldopa
Treat rebound hypertension from clonidine with
Phentolamine - non selective alpha blocker
B1 agonist
doButamine
Beta 2 agonist
Salbutamol
Albuterol
Salmetrol - long acting
Acute heart failure
Septic shock
Task: increase CO
B1 and D1 agonist
ie doButamine - b1; dopamine d1, b1
Hypertension
Glaucoma
Goal: decrease BP
Alpha 2 agonist
Uterine smooth muscle relaxation
Bronchodilation
B2 agonist
Non selective alpha blockers
Phenoxybenzamine - presurgical pheochromocytoma
Phentolamine - alpha 2 antidote for rebound hypertension
Alpha 1 blockers
“-zosin”s
Tamsolusin - selective for prostatic smooth muscle
Selective beta 1 blockers
BEAM
Betaxolol
Esmolol
Acebutolol
Metoprolol
Flow of aqueous humor
Ciliary body -> posterior chamber -> anterior chamber angle -> pupil -> anterior chamber -> trabecular meshwork -> canal of Schlemn -> uveoscleral veins
Glaucoma tx
Decrease secretion of aqueous humor from ciliary epithelium
Apraclonidine Alpha 2 agonist
Timolol Beta blocker nonselective
Mannitol
Acetazolamide/Dorzolamide Carbonic anhydrase inhibitor
Glaucoma meds
Ciliary muscle contraction opening trabecular meshwork, increasing outflow
Cholinomimetics
Pilocarpine. - direct ie an analog of ACh
Physostigmine. - indirect ie inhibit AChE
Glaucoma meds
Increase outflow through canal of Schlemn
Latanoprost - prostaglandin
Increased outflow via uveoscleral veins
Epinephrine