Drugs Flashcards
Cyclosporine
- Calcineurin inhibitor–> suppresses cytokine expression –> decreased T helper cell function –> inhibits IL-2
- Effective in 3-7 days
- Activates platelets
- Requires blood monitoring
Side Effects: GI signs, Gingival hyperplasia, hepatotoxins, secondary infectinos
Cholinomimetic Drugs
Ranitidine & Nizatidine –> inhibit AchE –> promotes gastric emptying
Bethanechol –> binds muscarinic receptors –> effect motility throughout the GIT
Proton Pump Inhibitors
Irreversibly inhibit H-K ATPase on luminal side of the parietal cell
V Tach treatment
SPAM!
- Sotalol
- Procainamide
- Atenolol or Amioderone
- Mexilitine
Verapmil
Calcium channel blocker
(less effect on HR compared to diltiazam)
Metoclopramide
- Peripheral 5HT3 Antagonist –> block CRTZ
- Peripheral 5HT4 Agonist
- Central dopaminergic antagonist: crosses BBB–> blocks CRTZ (may have decreased effectiveness in cats)
- Increased doses promote gastrokinesis
light sensitive
Renal clearance–> if decreased clearance may see hallucinations, frenzied activity, hyperactivity
DDAVP
Desmopressin Acetate
Primary V2 receptor action
- Increased vWF release increased FVIII
- Increases tPA
- Increased ADH activity
*Ideal if vWD type I & hemophilia A (decreased FVIII)
- Helps in uremic coagulopathy and liver disease
IV only no PO bioavailability (nasal product SQ)
Cisapride
5HT4 Agonist –> most effective prokinetics
- increased gastric emptying & chronic constipation
- IncreSed LES pressure
**Doesnt cross BBB
**Ineffective against striated muscle–> not helpful for mega esophagus
**Macrolides may inhibit
-Metabolized by P450 enzymes
-Cardiac conduction issues in humans
NK1 Antagonist
Cerenia
- Blocks action of substance P in CNS & at peripheral NK1 receptors in GIT
-1st pass metabolism in liver –> increased bioavailability IV
Puppies<11 wks–> BM hypoplasia
Aspirin as antithrombotic
- Irreversible blockade of plt COX-1–> platelet cannot make new COX since no nucleus
- ATE risk
- 2-3 days before effective in dogs
**Not recommended in cats due to decreased efficacy
tPA
Tissue Plasminogen Activator–> primary activator in vivo
- Does not bind circulating plasminogen normally–> but can at high doses
**$$
Mycophenolate
- Inhibits inosine monophasic dehydrogenase –> suppresses B & T Cells
- Effective 3-7 days
- Hepatic conversion
Side Effects: GI signs, lymphopenia, secondary infections
Volume of distribution
- Amount of abx in circulation & surrounding tissues ESP interstitial space
- High Vd = spread to many sites & [peak] at site of infection lower (except in UTIs with drug renal clearance)
- Hydrophillic drugs have increased Vd with critical illness (due to vascular dysfunction, fluid exvasiation)–> decreased abx at site of infection
Pharmacodynamics
Effect drug has on body and infecting pathogen
pharmokinetics
PK
- Effect body has on the drug
*extremely variable in critically ill patients
- affected by volume of distribution & drug clearance
Drug Clearance
Volume of plasma completely cleared of drug per unit time
- Lipophilic –> hepatic
- Hydrophilic –> renal
Motilin Receptor Agonist
Erythromycin –> stim motilin receptor–> increased LES pressure & peristalsis in large and small intestine
Calcitonin
Decreases Ca in 2-3 hours
**ER use
Zinc for liver
Decreased GI absorption of copper (binds in GIT)
N-Acetylcysteine
- Replenishes cellular cysteine and glutathione concentrations
- May stabilize RBC glutathione
** Good for toxicities & hepatic lipidosis
Post Synaptic alpha1 & presynaptic alpha2 agonist
Vasoconstriction
- Arterial vasoconstriction may increase afterload and impede tissue perfusion
- Venous vasoconstriction impedes VR if too increased
Augments ectopic pacemaker activity
**May increased BG and lactate (decreased insulin secretion and glycogenolysis)
Bethanechol
Parasympathetic agent–> stimulates cholinergic/muscarinic receptors for treatment of detrusor atony
*Urinary bladder contraction increased by PNS inpute
Leflunomide
- Inhibits dihydronotate dehydrogenase–> effects B & T cellls
*Inhibits S phase
Side effects: GI signs and myelosuppression
Grehlin & MOtilin
Grehlin (entyce) & motilin migrating motility complete in stomach –> stimulate GI motility, increase gastric emptying & gastric hunger
**Erythrimycin motili receptor agonist at microbial ineffective dose
Protamine
Reverse anticoagulent effects of heparin
Adverse reactions: systemic hypotension & anaphylaxis with repeat administration esp
Platelets on protamine insulin –> severe pulmonary hypertension
Yunnan Baiyo
Main active ingredient: Pseudoinseng root
dose dependent effect on platelet activation
No adverse effects reported but no quality control
Cabergoline
Dopamine antagonist
May be used with PGF2alpha analogs for pyometra
Causes luteolysis by reducing prolactin
Vitamin K antagonists
And monitoring
Ex: warfarin, coumarin, coumadin
- Inhibits vitamin K epoxide reductase –> FII, F VII, IX, & X + prostin s-c
**Procoagulant phase dose adjusted based off PT or INR2-3
Factor Xa Inhibitor
Rivaroxaban or Apixapan
Phenobarbital
- Prolongs opening of GABAa receptor–> increased Cl movement
- Inhibit glutamate & Ca Channels
- metabolized inthe liver
- 25% renal excretion
**Hepatotoxicity: Risk increased with serum concentration >40 mcg/ml
Bisphosphanates
Inhibits osteoclast function and promotes apoptosis
Inhibiys normal and abnormal bone reabsorbs
ie pamidronate, zoledronate –> takes a few days to work
Ketamine
NMDA noncompetitive antagonist–> NMDA receptor is excitatory receptor in N cells of dorsal root of spinal cord and thalamus
- Neuroprotective after reperfusion of ischemic tissues
Side Effects hallucinations, light headedness, inebriation
V1B Receptor
Located in Pituitary
ACTH release
Benzodiazepines
MOA: Primarily facilitates increase in GABA’s inhibition effects
Secondary MOA is antagonize serotonin and turnover ACH in CNS
*Diazepam: not water soluble –> IN, IV
- Absorbs plastic
*Midazolam: water soluble –> IM & IV
- Shorter half life
Side effects: dysphonia/excitatory signs, delayed awakening, seizures from acute benzo withdrawal
Keppra
MOA: Binds to the synaptic vesicle protein (SV2A) –> decrease neurotransmitter release from preganglion
- Urine excretion
Side Effects: salivation IV doses >1200mg/kg/day
Potassium Bromide
MOA: hyperpolarization of neuron by Br ions intracellularly through Cl channels
Excreted unchanged in urine
Reabsorbed via Cl channel in renal tubules–> diet changes may effect clearance
** Not recommended in cats: FATAL PNEUMONITIS
**Side effects: neuro deficits, PU/PD, vomiting, pancreatitis, upper and lower motor neuron deficits with increase in [Br-]
Where is V1A receptor
On vascular smooth muscle of kidney, pancreas, hepatocytes, thyroid, bladder, spleen, skeletal M & platelets
-At high doses: Cause vasoconstriction
- At low doses: vasodilation in cerebral, renal, pulmonary and mesenteric vessels
MOA V1a Receptor
Gq protein activation of phospholipase C & phosphoinositide pathways –> activate voltage gated Ca channels
- Also inactivates K-ATP channels –> opens voltage gated Ca channels –> increased cytosolic Ca2+
- Reduced blood flow to the inner renal medulla –> limits AVP there –> selective efferent arteriolar contraction–> increase GFR
V2 receptors
ON renal collecting duct, endothelial cells, platelets and vascular endothelium
Effects: increase water permeability, increase vWF release, stimulate aggregation, vasodilation
MOA V2 receptors
Located at basolateral membrane of distal tubule & principle cells of cortical and medullary collecting ducts
-Coupling Gs signalling pathway –> increased intracellular cAMP –> fusion of aquaporin-2 vesicles –> increased free water reabsorption
- Increased release of vWF & FVIII from endothelial cells
- DDAVP is V2R agonist
Recombinant FVIIa
For hemophilia A (FVIII deficiency) & B (IX deficiency)
- HemoA patients may also have impairment of extrinsic pathway (TF + FVII)
HIgh doses (10x normal) can compensate for lack of F VIII & IX
** hypersensitivity reactions and $$ inhibit use
Dantrolene sodium
Binds ryanodine receptor to depress excitation-contrqaction coupling in skeletal m
*specific treatment for malignant hyperthermia
LMW heparin
Ex: enoxaparin, dalteparin
- BTW 25-30% molecules can bind BOTH antithrombin and FIIa
- Exert primary effect on FXa–> decreased hemorrhagic events compared to UFH
- Not protein bound –> dont bind endothelial cells
** excreted by kidney
- Protamine sulfate only partially reversed
Tranexamic Acid
Competitive inhibition of plasminogen activation (& noncompetitive of plasmin at high doses)
Competitive inhibitor activation of trypsinogen and enterokinase
6-10x more potent that aminocaproic acid
**Excreted unchanged in urine
Adverse Effects: GI & hypotension if given fast
Epsilon aminocaproic acid
Competitively inhibits plasminohen activation & at high doses inhibits plasmin directly
Renal excretion
Adverse Effects: GI & hypotension if given fast
Aminopentamide
Anticholinergic with some anti-emetic effects
Unclear if MOA due to cholinergic receptors in vomiting center or upper GI (Vagus N)
**not as effective as other 5HT2 or antihistamines
Trientine
Chelates Copper –> seems to chelate serum stores greater than tissue stores
Vitamin E
Antioxidant activity by protecting phospholipids from oxidative injury by scavenging ROS
Liver Dz
D-penicillimine
Chelates heavy metals and allows urinary excretion
May lead Cu deficiency –> microcytic hypochromic anemia
Antifibrotic and immunomodulatory properties