week 1

Pharmacy

A branch of the health sciences that deals with preparation, dispensing, proper utilization of drug

Medicine

treats, cure, prevent or diagnose a disease

Pharmacology means

the study of drugs

pharmacology

body of knowledge concerned with the action of chemicals on biologic systems

drugs

chemical substance when administered to a living organism produces a biological effect

what are drugs used for

used to alter bodily function \n  covers herbal medications

medical pharmacology

concerned with the use of chemicals in the prevention, diagnosis, and treatment of disease, especially in humans

Toxicology

concerned with the undesirable effects of chemicals on biologic systems

what are two pillars of pharmacology

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* Pharmacokinetics
* Pharmacodynamics

Pharmacokinetics

Pharmacokinetics (PK) is defined as the movement of drugs through the body

Pharmacokinetics effects what

* describes the effects of the body on drugs
* e.g., absorption, metabolism, excretion, elimination etc

Pharmacodynamics

Pharmacodynamics (PD) is defined as the body's biological response to drugs

Pharmacodynamics affects what

* denotes the actions of the drug on the body
* such as mechanism of action and therapeutic and toxic effects

what are drug classification

 Effect \n  Chemical origin (precursor) \n  Receptor \n  Chemical structure

what does the mnemonics LEARN mean

Listen, Explain, Acknowledge, Recommend, and \n Negotiate

what does the mnemonic RESPECT mean

Rapport, Empathy, Support, Partnership, Explanations, cultural competence, and Trust

drug classification based on effect

 Blood thinners \n  Anti-inflammatory

Limitation

* Side effects
* Drug interactions
* Similar effects BUT act on different receptors

Do Blood thinners actually thin the blood

NO

how do blood thinner help blood vessel

Help blood flow smoothly through blood vessels and work to reduce a person’s risk of forming \n blood clots

can blood thinner break up existing clots

* Blood thinners do not dissolve or break up existing clots.
* But they can prevent existing clots from getting large

what are the two types of blood thinner

anticoagulants and antiplatelet drugs

Examples of anticoagulants

Heparin \n Lovenox (Enoxaparin) \n Pradaxa (dabigatran) \n Eliquis (apixaban) \n Coumadin (warfarin) \n Xarelto (rivaroxaban) \n Savaysa (edoxaban)

examples of antiplatelet drugs

Plavix (clopidogrel) \n Effient (prasugrel) \n Brilinta (ticagrelor) \n Persantine (dipyridamole) \n Aspirin

Analgesics

are drugs that relieve pain without causing loss of consciousness

two classification analgesics

* non-narcotic analgesics (e.g., acetaminophen, ibuprofen)
* narcotic analgesics (e.g., morphine, codeine).

classification of precursor molecules

* eicosanoids
* opiates
* opioids

what is the difference between opiates and opiods

one is made in the lab and the other is natural

Eicosanoids is derived from

eicosapentaenoic acid (arachidonic acid)

examples of eicosanoids

prostaglandins, leukotrienes, and thromboxanes

is there information of the effects of eicosanoids

No information on actual effects

where is opiates are derived from

Derived from opium poppy, Papaver somniferum

example of opiates

Opium, heroin, morphine, and codeine

do opioids work on the same receptors as opiates

* work on same receptors as opiates but are NOT opium derivatives

opioids

\n  chemical compounds not derived from natural plant matter

Receptor occupancy

\
Stimulate or block receptor

subclassification of receptor occupancy

Agonist versus Antagonist/Blocker

Sympathetic Nervous System classification

Adrenoreceptor

Sympathetic Nervous System subclassification

 Adrenaline \n  Noradrenaline

agonist

Activate receptors in the body and produce a therapeutic effect

Agonists example

Examples include morphine (an opioid agonist) and albuterol (a beta-2 agonist)

antagonists

block the action of agonists

antagonists example

Examples include naloxone (an opioid antagonist) and flumazenil (a benzodiazepine antagonist)

Enzyme inhibitors

Block the action of enzyme in the body

enzyme inhibitors example

Examples include acetylcholinesterase inhibitors (used to treat Alzheimer’s disease) and angiotensin- \n converting enzyme (ACE) inhibitors (used to treat hypertension)

ion channel blocker

Block the flow of ions through ion channels in the body.

ion channel channels blockers example

Examples include calcium channel blockers (used to treat hypertension) and sodium channel blockers \n (used to treat epilepsy)

Adrenoreceptors types

* alpha and beta (a1,a2, b1,b2)
* agonist versus antagonists

Drugs may work on multiple receptors

* labetalol (Normodyne) \n  Blocks adrenoreceptor
* diphenhydramine (Benadryl) \n  common histamine receptor blocker \n  blocks Histamine receptors \n  H1 \n  blocks muscarinic acetylcholine receptors.

receptors

Receptors largely determine the quantitative relations \n between dose or concentration of drug and pharmacologic \n effects

what are receptor responsible for responsible

Receptors are responsible for selectivity of drug action

what do Receptors mediate

\
Receptors mediate the actions of pharmacologic agonists and antagonists

Example of receptor types

 Ion-channel receptors (Ionotropic) \n  G-Protein coupled receptors (Metabotropic) \n  Kinase-kinked receptors \n  Intracellular receptors (Cytosolic) \n  Enzymes as receptors \n  Voltage gated ion channel

pharmacokinetics

Fate of substances administered externally to a living \n organism

what is pharmacokinetics

\
is the science of the kinetics of drug \n absorption, distribution, metabolism, excretion, and \n clearance (elimination)

how is the body affected Pharmacokinetics

Pharmacokinetics is what the body does to the drug

Selectivity

defines the ability of the receptor to distinguish between drugs and has the same \n implications as specificity

Specificity

measure of a receptor’s ability to respond to a single ligand

what is the difference between low specificity vs high specificity

low specificity generally results in physiologic responses not targeted or intended by the \n drug

example of specificity

 side effects are a good example \n  E.g., sildenafil (Viagra; Pfizer)

Efficacy

maximum response achieved from a drug

what does it mean to have a high affinity

A high affinity is generally associated with a lower dose requirement

Affinity

Affinity defines the strength of attraction between the drug and its receptor

How does efficacy affect the body

interaction (e.g., absorption, metabolism, and excretion) of the drug in the body may \n alter the relative bioavailability and change the theoretic effect of the drug.

Potency

Potency describes the relationship between the drug dose and the magnitude of the effect

what does high potency mean

High potency induces a strong effect with a low drug dose

pharmacodynamic properties

 Affinity \n  Potency \n  Efficacy \n  Specificity \n  Selectivity

Pharmacodynamics

Pharmacodynamics is what a drug does to the body

example for pharmacodynamics

A typical example of pharmacodynamics is how a drug interacts \n quantitatively with a drug receptor to produce a response (effect)

what is the concept behind pharmacodynamics

The concentration or dose of drug required to produce a therapeutic \n effect in most of the population usually will overlap with the concentration required to produce toxicity in some of the population

What are the BAN and INN name for Sulfamethoxazole and trimethoprim combination?

* Cotrimoxazole - BAN
* trimethoprim-sulfamethoxazole- INN, BAN, and USAN

What are the BAN, USAN, and INN name for Acetaminophen?

USAN \n Pain, fever \n INN, BAN \n Paracetamo

What are the BAN, USAN, and INN name for Cephalexin?

USAN \n Antibiotic \n INN \n Canada \n Cefalexin \n But sold as Cephalexin

What are the BAN, USAN, and INN name for Acyclovir?

• USAN \n potent antiviral drug \n • INN \n aciclovir \n • Canada \n generic name \n acyclovir

What are the BAN, USAN, and INN name for Epinephrine?

USAN and INN \n • BAN \n adrenaline \n • Canada \n Epinephrine \n • adrenaline often \n used

What are the BAN, USAN, and INN name for Pethidine?

• INN, BAN \n Opiate \n • USAN, Canada \n Meperidine

Generic name

* Exclusive name listed in pharmacopoeias \n  Publications listing the official names of drugs and describing how the drugs are prepared

The United States Adopted Names (USAN) Program

 assigns generic (nonproprietary) names to all active drug ingredients in US \n  American Medical Association (AMA), the United States Pharmacopeial Convention (USP), and the American Pharmacists \n Association (APhA

World Health Organization (WHO)

 publishes recommended International Nonproprietary Names (INN) for active drug ingredients \n  not a substitute for a USAN

British Approved Names (BAN)

nonproprietary name or generic name for an active pharmaceutical ingredient (API) for use in the UK \n  distinctive names for use with medicines in the UK \n  harmonized with the English form of the recommended international nonproprietary name (rINN)

Canada

* INN is typically used
* sometimes the USAN

Chemical name

 A unique name given to a compound \n  by the International Union of Pure and Applied Chemistry (IUPAC). \n  The IUPAC nomenclature is based on rigid rules

what are the Pros and Cons for chemical name

Pros \n - the structure of the molecule can be recreated if its name is known \n Cons \n - needs a solid background in chemistry to understand \n - the names tend to be awkward and long

Example of diazepam with chemical, generic and proprietary name

Chemical name for diazepam is: \n  7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-,1,4-benzodiazepin-2-on

\n  Generic name is diazepam \n commonly used sedative.

\n  Proprietary or tradename \n Each company can have a different tradename (brand name) for the same drug the best \n known proprietary or tradename for diazepam is Valium (from the pharmaceutical company \n Roche), but other proprietary names for diazepam include Valpam (Arrow), Antenex \n (Alphapharm) and Ducene (Sauter).

Chemical name

* used by chemists to describe the chemical structure
* name given by International Union of Pure and Applied Chemistry (IUPAC)

Generic name

* used by pharmacologists \n
* also known as non-proprietary name to distinguish it from the proprietary or trademark name.
* Exclusive chemical name under which it is listed in major pharmacopeias

Trade name

* used by the pharmaceutical companies.

G protein-coupled receptor (GPCR) agonists and antagonists

* Family of cell surface receptors that mediate numerous physiological responses in \n the body, such as neurotransmission, hormone secretion, and immune response

GPCR is important

* Drugs that activate or inhibit GPCRs can have significant therapeutic effects, such \n as pain relief or reduced inflammation.

Enzyme inhibitors:

Enzymes are molecules that catalyze biochemical reactions in the body, and their \n inhibition can prevent or modify the course of a disease

Enzyme inhibitors can be classified into two categories

irreversible inhibitors and reversible inhibitors

irreversible inhibitors

Irreversible inhibitors bind covalently to the enzyme

reversible inhibitors

reversible inhibitors bind non-covalently and can be either competitive or non-competitive.

Molecular target

Drugs interact with biomolecules such as lipids, proteins, nucleic acids, and carbohydrates

Biomolecules are known as

target molecules or drug targets

How do similar drug structure affect the target

\
Drugs with similar structures may have a similar mechanism of action on targets

example of molecular target

* Aspirin works by blocking a certain natural substance in the body to reduce pain and \n swelling
* Aspirin is also used to reduce fever and relieve moderate pain from conditions such as \n muscle aches, toothaches, the common cold

Chemical structure

* Share common structural features
* Have similar pharmacological activity

example of chemical structure

Sulfonamides

Cyclooxygenase (COX)

involved in the conversion of arachidonic acid to prostaglandin H2