Pharmacology Flashcards
Branch of medicine concerned with USE, EFFECTS, and MODES OF ACTION of drugs
Pharmacology
Concerned with EFFECT OF DRUGS and MECHANISM OF ACTION
Pharmacodynamics
Concerned with MOVEMENT of drugs
Pharmacokinetics
Movement of Drugs
Absorption
Distribution
Metabolism
Excretion
Water Soluble Vitamins
Vit B
Vit C
Lipid Soluble Vitamins
Vitamin: A D E K
Study of drug’s HARMFUL effects
Toxicology
Example of drugs that reverses toxicity
Activated Charcoal
Syrup of Ipecac
Accumulation of drug because it cannot be excreted by the body
Cumulation
Drugs CONTRAINDICATED for px with GLAUCOMA
Cholinergics
Anti-Cholinergics
Diazepam
Most allergenic drug
Penicillins
Study of DAMAGE TO FETUS
Teratology
Study of DRUG DOSAGE
Posology
Routes for administration of drugs
Enteral
Parenteral
Inhalation
Enteral administration
Oral
Rectal
Parenteral administration
Intradermal Intravenous Subcutaneous Intramuscular Intrathecal
Fastest route of drug administration to reach the brain
Inhalation
Intradermal angulation
0-15 degrees
Intravenous angulation
35 degrees
Subcutaneous angulation
45 degrees
Intramuscular angulation
90 degrees
Drug properties that influence absorption
Weak acid
Weak base
Amount of drug that reaches the systemic circulation
Bioavailability
Common site for Intravenous Medications
Antecubital Region
Common sites for intramuscular administration
Pedia - Vastus lateralis
Adults - Dorsogluteal
Factors that affect bioavailability of drugs
Solubility
Route
First-Pass effect
Phenomenkn where concentration of orally taken drugs is REDUCED before reaching systemic circulation
First-Pass Effect
Types of drug according to distribution
Free Ionized Drug
Bound Drug
Temporary Storage of Drugs
Adipocytes
Blood
Tendency of a substance to separate or dissociate from binding
Dissociation Constant
Metabolic Pathways
Liver
Plasma
Types of liver enzymes
Microsomal
Non-microsomal
Function of liver in metabolism
Lipid soluble to lipid insoluble
Active drug to inactive
Prodrug to active
Aspirin is converted to
Salicylates
Codein is converted to
Morphine
Types of local anesthesia
Amide
Esters
Drug of choice if allergic to amide and ester
Diphenhydramin Hydrochloride
Amide exception
Articaine
Ester excemption
Piperocaine
Sites for excretion
Kidney Lungs Breast milk Bile Large intestine Saliva Sweat
Plasma enzyme
Plasma pseudocholinesterase
Drugs metabolized in the plasma
Ester LA
Succinylcholine
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-effect (dose-response) relationship
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Antagonist that competes with receptor sites of agonist
Competitive
Antagonist that does not compete with agonist and has own receptors
Non-competitive
Antagonist that results in dec potency
Competitive
Antagonist that results in dec efficacy
Non competitive
Antagonist of narcotics
Naloxone
Naltrexone
Antagonist of benzodiazepines
Flumazenil
Acts as agonist and antagonist
Partial agonist
Drugs specifically bind and interact with their receptor
Stucture action relationship
Theories of structure action relationship
Clark’s Occutoational Theory
Paton’s Rate Theory
Drug effect is proportional to the number of receptors occupied
Clark’s occupational theory
Drug effect is proportional to rate at which drug and receptor combine
Paton’s Rate Theory
Accdg to Payton
Associates quickly, dissociates immediately; faster rate of binding
Agonist
Accdg to Payton:
Associates but dissociates slower; slow rate of binding
Antagonist
Properties of Diphenhydramine HCL
LA
H1 Blocker
Sedative
Slight cholinergic effect
LA metabolized in the liver
Amide
LA metabolized in plasma
Esters
Time required for drug to reduce half of its initial value
Half life
Rate at which drug is removed from the body
Clearance
Types of clearance
Zero order kinetics
First order kinetics
Constant clearance, not constant half life
Zero order kinetics
Not constant clearance, constant half life
First order kinetics
Drug which has more chances of cumulation
Zero order kinetics
Dosage of drug needed to produce an effect
Potency
Effect of drug
Efficacy
How well drug can be used in the real world
Effectiveness
Effect of drug are dose dependent
Dose-effect relationship
Dose-response responses
Graded dose effect curve
Quantal dose effect curve
Degree of response of a single biological unit
Graded dose effect curve
Relationship bet increasing drug dosage and percent of population that shows drug’s pharmacological effect and lethal effect
Quantal dose effect curve
Formula for therapeutic index
TI= LD50/ED50
Median effective dose
ED50
Median lethal dose
LD50
Targets of drug action
Receptors
Enzymes
Drug acting as physical or chemical agents
Receptors for narcotics
Mu
Kappa
Delta
Receptor for pilocarpine
Muscarinic
Drug properties
Affinity
Intrinsic activity
Ability of drug to bind to target sites
Affinity
Ability of drug to produce an effect
Intrinsic activity
Receptor acting drugs
Full agonist
Antagonist
Partial agonist
Types of antagonist
Competitive
Non-competitive
Competes with receptor sites of agonist
Competitive
Does not compete with agonist and has own receptors
Non-competitive
Results in dec potency
Complete