Pharmacology I Flashcards
Branch of medicine concerned with the uses, effects and modes of action of drugs
Pharmacology
Branch of pharma concerned with EFFECTS OF DRUGS and MECHANISM of their action
Pharmacodynamics
Branch of pharma concerned with MOVEMENT OF DRUGS within the body
Pharmacokinetics
Process of pharmacokinetics
ADME Absorption Distribution Metabolism Excretion
Study of drug’s harmful effects
Toxicology
2 drugs that prevent toxicity
Activated charcoal
Syrup of Ipecac
Absorption of drug starts in….
Small intestine (jejunum)
Activated charcoal has a property called ____
Adsorption - stick to different toxins
Accumulation of drug bec it cannot be excreted by the body
Cumulation
Cumulation is associated with (2)
Liver damage
Kidney damage
Drugs contraindicated for glaucoma
Diazepam
Anticholinergic drugs
Most allergenic drug
Penicillins
Study of damage to fetus during development
Teratology
Study of drug dosage
Posology
Teratogenic drug (2)
Tetracyclines
Thalidomide
Process of drug uptake from site of administration towards the bloodstream
Absorption
Route of administration during absorption (3)
Enteral
Parenteral
Inhalation
Most common site of drug administration
Oral
Common site of IV
Antecubital region
Most common site for IM
Vastus lateralis
*Bypasses membranes (straight to circulatory)
IV
Fastest route if target site is BRAIN
Inhalation
Type of route with slow and least absorption
Intradermal
Weak acids are attracted to ____
Weak bases are attracted to ______
Higher pH levels (6 to 7.4)
Lower pH levels (8 to 7.4)
Amount of drug that reaches the circulatory system after administration
Bioavailability
Drug solubility
Slightly hyrophilic
Largely hydrophobic
Phenomenon of drug metabolism whereby the cxn of orally taken drugs is reduced before reaching the systemic circulatory
First pass effect
Ability of drug to move from circulatory system into their target sites
Distribution
Free floating drugs
Free ionized drug
Bounded to plasma proteins
Bound drug
Tendency of substance to separate or dissociate from its binding
Dissociation constant (Kd)
**Most important microsomal liver enzyme
Cytochrome P450
Example of PRODRUGS (3)
Aspirin or acetylsalicylic acid (asa) - salicylates
Codeine - morphine
Alcohol - ethanol
Drugs metabolized in liver
Amide LA
Most drugs
Drugs metabolized in plasma
Ester LA
Succinylcholine
***for laryngospasm
Succinylcholine
Drug used if px is allergic to both amide and ester
Diphenhydramine HCL
*Plasma enzyme
Plasma pseudocholinesterase
Liver enzyme
Microsomal enzyme
Non microsomal enzyme
Time required for a drug to reduce half of its initial value
Half life (t1/2)
Rate at which the active drug is removed from the body
Clearance
Amount of drug eliminated is CONSTANT and is NOT dependent on the cxn of drug in plasma fluid
Zero order kinetics
Amount of drug eliminated is DEPENDENT on the cxn of drug in plasma fluid
Most drugs
First order kinetics
Drug that has more chances of cumulation
A. Zero order kinetics
B. First order kinetics
C. Same
A.
Dosage of drug needed to produce an effect
Potency
Refers to the EFFECT OF A DRUG
Efficacy
Maximum effect of a drug where no effect is added even though drug dose is increased
Maximal effect or ceiling effect
Curve that describes the degree of response of a single biological unit to a given drug dose
Graded dose effect curve
Curve that describes the relationship bet increasing drug dosage and % of the population
Quantal dose effect curve
Absorption start from what organ
Small intestine (jejunum)
What organ convert drugs into water soluble
Liver (metabolism)
Safe for pregnancy
LA
Analgesics
Sedative hypnotics
Slow and least absorption route
Intradermal
IM site
Vastus lateralis
Gluteus maximus
Deltoid
Site for gluts
Superolateral or outer lateral corner
Organ responsible for first pass effect
Liver
Lower Dissociation constant = slower distribution = low or high tendency to separate to drug
Longer or shorter duration
Slow effect or fast
Slow onset or fast
Longer
Slow
Slow
Function of liver in drug metabolism
Lipid sol to water sol
Converts active to inactive form
Converrs prodrugs to active form
Most common topical anesth
Benzocaine
LA metabolized by both liver and plasma
Articaine
Major organ for excretion
Kidney
Example drug of zero order kinetics (3)
Alcohol
Phenytoin
Aspirin
Dose of drug that has therapeutic effect in 50% of population
Medial effective dose (ED50)
Dose of drug that has lethal effects in 50% of population
Medial lethal dose (LD50)
*Therapeutic index formula
LD50/ED50
TLE
Targets of drug action (3)
Receptors
Enzymes
Drug acting as physical or chemical agents
Ability of drug to bind to its target site
Affinity
Ability of drug to produce an effect after binding to its target site
Intrinsic activity
Part of body where drugs interact to produce their effects
Receptors
Elicits maximal response by activating all or portions of the receptors
Full agonists
Instrinsic activity of 0
Antagonist
Competes with receptor sites of agonists
Results in dec potency
Competitive antagonists
Example of competitive antagonist
Belladona alkaloids
Belladonna alkaloids (2)
Atropine
Scopolamine
Competes against cholinergic drugs
Belladonna alkaloids
Antagonist that has its own receptor and doesnt compete
Result in dec efficacy
Non competitive Antagonist
Naloxone is an antagonist of what drug
Narcotics
Flumanezil is an antagonist of what drug
Benzodiazepines
Produces less maximal response even all receptors are occupied
Partial agonist
Acts as an agonist and antagonist
Partial agonist
2 theories of structure action relationships
Clarks occupational theory
Paton’s rate theory
Theory wherein drug effect is PROPORTIONAL to the number of RECEPTORS OCCUPIED
Clark’s occupational theory
Drug receptor relationship that has affinity and intrinsic activity
Full agonists
Drug receptor relationship that has affinity but no intrinsic activity
Antagonist
Drug receptor relationship that has affinity but lesser intrinsic activity compared to agonist
Partial agonist
Clark’s occupational theory aka
Occupational theory
Drug effect is proportional to RATE at which the DRUG and RECEPTOR combine
Paton’s Rate theory or rate theory
Drug associates quickly and disassociates immediately to the receptor to be able to reassociate again
Agonists
Drug associates but dissociates much slower therefore reassociation to the receptor is also slower
Antagonist
Sedative hypnotics are used for (3)
Sedation
Hypnosis
Muscle relaxation
Types of sedation
Minimal
Moderate
Deep
Type of sedation wherein px is awake and relaxed
Minimal or conscious sedation
Type of sedation with feeling asleep but can follow commands
Moderate sedation
Type of sedation that is asleep but can be awaken
Deep sedation
Medically induced coma
Gen anesthesia
Two types of amnesia
Anterograde
Retrograde
Type of amnesia that doesn’t form new memories
Anterograde
Type of amnesia wherein old memories are forgotten
Retrograde amnesia
Classification of sedative hypnotics
Barbiturates
Non barbiturates
Active ingredient of barbiturates
Barbaric acid
Classification of barbiturates (4)
Ultra short acting
Short acting
Intermediate acting
Long acting
Ultra short acting drugs (2)
Thiopental
Methohexital
TM - ultrashort ultramura
Guedel’s stage of gen. anesthesia (4)
Stage 1 - amnesia and analgesia
2 - delirium
3 - surgical anesth
4 - respiratory depression
Short acting barbiturates(2)
Secobarbital
Pentobarbital
(SSPENT - Short Seco Pento)
Intermediate acting barbiturates(2)
Amobarbital
Butabarbital
(AmBuy)
Long acting barbiturates (3)
Phenobarbital
Mephobarbital
Primidone
Barbiturates for epileptic seizures
Long acting
Non barbiturates(4)
Chloral hydrate
Flurazepam
Ethanol
Diphenhydramine
Non barbi commonly used in Pediatrics
Chloral hydrate
Specific receptor of narcotics
Mu kappa delta
Specific receptors of cholinergic (para)
Muscarinic receptors
Reduce action of cholinesterase to improve muscular contraction
Anti cholinesterase
*anti cholinesterase drug is used for what dse
Myesthenia gravis
Drug properties (2)
Affinity
Intrinsic Activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Naloxone or Naltrexone is as ANTAGONIST of what drug
Narcotics
Flumanezil is an ANTAGONIST of what drug
Benzodiazepines
Used for induction of gen anesth
Ultra short acting barbiturates
Stage 1 of gen anesth
Amnesia and analgesia
Unstable stage of gen anesth
Stage 2 -delirium
Most stable stage of gen anesth
Stage 3
Surgical anesth
Stage of gen anesth wherein it can happen if px is overdosed
Stage 4
Respiratory depression
Administration of chloral hydrate
Oral
Regulate sleep wake cycles
Reticular activating System (RAS)
Drug for lethal injection (3)
Thiopental
Pancuronium bromide
KCl
Drug uses (sedative - hypnotic drug)
Sedation
Induction of gen anesth
Insomnia
Anti seizure and anti anxiety
Adverse drug effects of sedative hypnotic drugs (4)
Drug dependence
Stimulates porphyrin production
Respiratory depression
Coma
Depressant drugs
SNAB KA
SEDATIVE HYPNOTICS
NARCOTICS
ALCOHOL
BENZODIAZEPINES
Never combine with other CNS depressant because it has ____ effect
Synergistic effect
1+1 = >2
Sedative hypnotics produces analgesia
T or F
False
Sedative hypnotics produces drug dependence
True
Naloxone and narcotics have ____ effect/drug
Antagonist
1+1=0
Demi Lovato
Anti convulsant drugs are used (3)
Anti epileptic or anti seizure
Antianxiety
Sedation
Type of seizures
Partial seizure
Generalize seizure
Seizure with abnormal activity in just one part of the brain
Partial seizure
Seizure where abnormal activity in all parts of brain
Generalize seizure
Seizure with absence of consciousness
Absence of movt for few seconds
AKA
Absence seizures
Petit mal seizure
Seizure wherein muscle are jerking for few seconds to few mins
Myoclonic
Seizure wherein there is muscle relaxation for few seconds to few mins
AKA
Atonic seizure
Drop seizure
Seizure wherein px is unconscious with muscle stiffness and jerking movt’s for few mins
Most common type
Tonic clonic seizures
Tonic clonic seizure aka
Grandmal seizure
Up to 5 mins
30 mins seizure aka
Status epilepticus
Repeated grandmal
DOC for tonic clonic and status epilepticus seizure
Diazepam
Phenytoin (if wala sa choice ung isa)
Ca channel blocker drugs
Nifedipine
Verapamil
Cyclosporine
Drug with gingival hyperplasia side effect
Phenytoin
Nifedipine
Verapamil
Cyclosporines
Doc for tic douloureux
Carbamezapine (Tegretol)
*Benzodiazepines that induce GA
Midazolam
Diazepam
Lorazepam
Most common benzodiazepines used for GA
Midazolam
Least common benzodiazepines used for GA
Lorazepam
Common drugs for anti seizure (5)
Benzodiazepines Phenytoin Carbamezapine Valproic acid Barbiturates
Anti anxiety drugs potentiates _____ receptors and ______ neurotransmitters
GABA
Inhibitory
Main use for phenytoin (2)
Anti seizure
Anti arrythmia
Active drug of benzodiazepines
Dimethyldiazepam
Diazepam is slowly and poorly absorbed in what route of administration
IM
Diazepam is greatly absorbed in (2)
Oral
IV
Adverse effect of Anti anxiety drugs
Severe sedation
Paradoxical excitement
Drug dependence
Respi depression
Drug induced gingival hyperplasia
Anti anxiety Drug uses
Anti convulsants
Preop sedation
Induction of gen anesth
Insomnia
Mild anticholinergic effect