Pharmacokinetics

Front 1

study of how drugs move into, through and out of the body

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Pharmacokinetics

Front 2

study of how drugs produce their effects in the body

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Pharmacodynamics

Front 3

Ideal range of a drug concentration within the body. Too much can be toxic, too little has no beneficial effects and can cause antibiotic resistance.

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Therapeutic range

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top end of normal therapeutic range

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Maximum Effective Concentration

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bottom end of normal therapeutic range before hitting the sub therapeutic range.

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Minimum Effective Concentration

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Amount of drug administered at one time.Units of mass such as grams, milligrams, or litres, millilitres.

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Drug Dose

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amount administered to animal at one time.

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dose

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amount to be given over entire treatment period

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dosage

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Time between administrations of separate drug dosages. e.g., BID, TID q4h

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dosage interval

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Random movement of drug molecules from high concentration to low. e.g, iso into the brain Movement continues down the concentration gradient until equilibrium is reachedNo energy required

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Passive diffusion

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Passive movement that requires a carrier molecule e.g., glucose moving into cellsNo energy required

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Facilitated Diffusion

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Movement that uses a special carrier molecule.Requires energyDrug can move against concentration gradient

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Active Transport

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small invagination in cell wall will surround particles and bring them into the cellDrug molecules engulfed by cell membrane- requires energy

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Pinocytosis

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Large invagination that brings larger molecules into cellalso requires energy

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phagocytosis

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4 steps of pharmacokinetics

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absorption

distribution

metabolism/biotransformation

excretion/elimination

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dosages designed to result in therapeutic concentrations based on ___ of the drug

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ADME

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movement from site to systemic circulation

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Absorption

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degree to which a drug is absorbed and enters the general circulation

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Bioavailability

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Rate of drug absorbed

amount of drug absorbed

distribution of drug throughout the body

drug metabolism or biotransformation

rate and route of excretion

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factors influencing the blood concentration levels of a drug

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Cells and cell membranes are phospholipids

Move quickly into extracellular fluid

absorb slowly if given SQ or IM

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Lipophilic

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Cells and cell membranes are phospholipids

Extracellular fluid is water and solutes

Move quickly into cells

absorbed quicker when given SQ or IM.

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Hydrophilic

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oral drugs should be

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lipophilic

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greater absorption(slower absorption)

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hypomotile

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less absorption(faster absorption)

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hypermotile

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blood circulating in the intestines must travel through the liver before returning to the system circulation through the hepatic portal system

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first pass effect

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liver recognizes some drugs as foreign substances

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xenobiotics

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movement of drug from the systemic circulation into tissues

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distribution

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math value that gives an estimate of the extent to which a drug is distributed throughout the body

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Vd

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the ______ Vd of a drug, the more tissues drug will penetrate. Because the drug gets distributed to many compartments in the body, the drug concentration in the blood will be lower

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larger

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______deliver the blood to the tissues from the bloodstream

_____ are lined by cells with fenestrations in between them

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capillaries

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lipophilic drugs are highly_______, dosage is based on this

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protein bound

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if animal has ____ protein level, the amount of free drug reaching tissue quickly will increase and could be toxic

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low

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drugs reach well perfused tissues easier- tissues with high blood flow or vasodilation

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perfusion of tissues

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Blood-brain barriervery tight junctions between capillary cellsno fenestration

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barriers

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drugs must be small or ___ to enter the brain

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lipophilic

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Brain has _____pumps that pump out drugs that enter. also found in testis and GIT

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P-glycoprotein

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drug molecules combine with parts of a cell to alter cell functioneffect on the cell could be depression, stimulation, irritation or death

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Receptors

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degree to which a drug produces desired response

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Efficacy

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tendency of a drug to combine with a receptor

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affinity

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high level of affinity and efficacy causes a specific action

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agonist

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less affinity and efficacy

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partial agonist

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drug that blocks another drug from a receptor

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Antagonist

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when drugs can be eliminated by the body

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metabolism/biotransformation

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altered drug molecule is called a ___

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metabolite

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Biotransformation results in a metabolite that is more ___ so it can be eliminated by kidney or liver

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Hydrophilic

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when lipophilic drugs diffuse back into circulation from ingest and return to liver it is called the

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enterohepatic

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drugs that require biotransformation to become activeprednisone to its active form prednisolone

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Prodrugs

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is a liver enzyme. It changes bilirubin into a form that can be removed from the body through the bile. It also changes some hormones, medicines, and toxins into non-harmful products.

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Glucoronyl Transferase

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Movement of drug molecules out of the body

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elimination

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most common routeoccurs via renal artery and the glomeruli through processes called filtration (passive) and active secretion

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renal elimination

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Passive process as blood flows through glomeruliSmall drugs not bound to proteins filter into bowman capsule and get removed in urine

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glomerular filtration

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Drugs that are actively secreted into urine results in drug being removed quicker which is beneficial if treating a UTI

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active secretion

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from the proximal convoluted tubule the filtrate moves into the loop of henlein the loop drugs can move passively from filtrate back into circulation through ______

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reabsorption

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passive process so drug must be in ____ form.

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lipophilic

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decreases blood flow into glomerulus- slower eliminationcould cause toxic levels and increases WTdehydration, blood loss, shock

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Hypotension

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decreased blood flow to kidney and liver- slower rate of elimination

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Congestive heart failure

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result in hypoalbuminemia or hypoproteinemia which results in less drugs being protein bound so these drugs are eliminated rapidly

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Liver disease

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Elimination of drugs by the liver. Drugs removed this way go into the bile

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Biliary excretion

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If drugs arrives in duodenum in a lipophilic form, it can be reabsorbed into the hepatic portal circulation back to the liver to be excreted by the liver again or reabsorbed back into systemic circulation

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Enterohepatic Cycle

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May result in drug having an effect on the body for a longer period of timeIf _____ is compromised by disease or old age, rate of elimination is reduced

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Liver Compromise

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Rate at which drugs leave the body is expressed as the drugs clearance or _____

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half-life eliminatiion

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The point at which drug accumulation and elimination are balanced

Peak and trough concentration should all be the same

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Steady State

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The point at which drug accumulation and elimination are balancedPeak and trough concentration should all be the same

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Withdrawal Time

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A measure of how safe a drug is

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Therapeutic Index

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The delay between the administration of a drug and when the effects of the drug are seen

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Latent Period

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unusual or unsuspected reaction is called an _________

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idiosyncratic drug reaction

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Severe and life threatening

Fluid in lungs- severe dyspnea

Swelling of respiratory tract

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Anaphylaxis

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less severe

swelling, hives, itchiness

Usually occurs within 2 hours of giving the drug but could take longer

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Urticaria

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Damage to DNA of a cell

In antibiotics or antifungals that work on bacterial cell DNA

Should be a warning on the label

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Carinogens

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Cause birth defects in pregnant animals

Fulvicin- anitfungal- missing limbs

Tetracycline- discolor teeth, bones

May not always state “dont use on pregnant animals”

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Teratogens

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TDM

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Therapeutic Drug Monitoring

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Periodically measure blood levels for certain drugs

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TDM

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Drugs may precipitate when mixed togetherValium and anything other than Diazepam

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Chemical/Physical

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Altered Absorption

Calcium will bind to many drugs and interfere with absorption

Altered Metabolism and Elimination

Dewormers and tranquilizers, anesthetics

Use the same enzymes to be metabolized

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Pharmacokinetic

Front 75

Interaction at the site of a drug actionAgonist and antagonists

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Pharmacodynamic