Pima - Pharmacology

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Oral

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Enteral
Oral, sublingual, rectal (GI)
any route of drug administration that involves absorption of the drug through the gastrointestinal tract

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Injectable

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Parenteral

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Topical

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skin or mucous membrane

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Inhalational

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Inspired directly into lungs for local (targeted) or systemic effect

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Receptor

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Cell structure that combines with a chemical or drug to change or enhance a cell function

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generic name

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a name assigned to a drug that can be used by anyone (non-proprietary)

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Official reference book of standards used by FDA

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US Pharmacopeia

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Entity that approves drugs in the USA

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Food and Drug Administration - FDA

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Three Phases of Drug Action

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Pharmaceutical Phase

Pharmacokineic phase

Pharmacodynamic phase

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Pharmaceutical Phase

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How the drug gets into the body

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Routes of administration

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Oral = Enteral
Injectable (Parenteral)
Topical
Inhalational

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Enteral

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Oral
Sublingual
rectal
Anything that goes through the GI tract

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Parenteral

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Injectable

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Topical

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skin or mucus membrane

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Inhalational

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Inspired directly into lungs for local (targeted) or systemic affect

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Pharmacokinetics

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What our body does to the drug

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Four steps of Pharmacokinetics

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Absorption
Distribution
Metabolism
Excretion

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Pharmacodynamic Phase

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What a drug does to the body physiologically.

Drugs may increase, decrease or replace enzymes, hormones or body metabolic functions

Drugs can only alter an existing function, they cannot create new responses

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Receptor

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Cell structure that combines with a chemical or drug to change or enhance a cell function

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Agonist

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a chemical or drug that binds to a receptor & creates an effect in the body

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Antagonist

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Chemical or drug that binds to a receptor & blocks agonists

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Syngergism

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Combined effects of 2 greater than if each given alone

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Tolerance

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Repeat usage same drug decreases intensity of response to a drug over time

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Sensory division of the Peripheral Nervous System

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Afferent - Nerve fibers carry information to the central nervous system

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motor division of the PNS

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Efferent - Nerve fibers carry impulses away from the CNS

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Two divisions of the Efferent division of the PNS

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Somatic nervous system - Voluntary - skeletal muscle

Autonomic nervous system - involuntary - cardiac and smooth muscle, glands

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Two divisions of the Autonomic Nervous System

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Sympathetic - fight or flight

Parasympathetic - rest & digest

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Autonomic Nervous System

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Controls many organs

Drugs that affect ANS affect many organs

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Adrenergic bronchodilators

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(specifically beta2-adrenoreceptor agonists) are inhaled medicines that help open up the air passages. They are used to treat asthma and chronic bronchitis. They dilate the bronchi by a direct action on the beta2-adrenoreceptors on the bronchial smooth muscle and relax the muscle.

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The three types of prescription bronchodilating drugs are

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β2-agonists (short- and long-acting)

anticholinergics (short-acting)

theophylline (long-acting)

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Anticholinergic bronchodilators

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(or muscarinic receptor antagonists) block the parasympathetic nerve reflexes that cause the airways to constrict, so allow the air passages to remain open. Muscarinic receptor antagonists bind to muscarinic receptors and inhibit acetylcholine mediated bronchospasm.

Anticholinergic bronchodilators are used more to treat chronic obstructive pulmonary disease than to treat asthma.

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Inhaled corticosteroids

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act locally in the lungs to inhibit the inflammatory process, which causes asthma. They are potent anti-inflammatory agents and effectively reduce asthma symptoms. Corticosteroids prevent asthma attacks and improve lung function. Inhaled corticosteroids may also be used to treat chronic obstructive pulmonary disease that has an asthmatic component.

Inhaled corticosteroids deliver the medicine directly into the lungs so a smaller dose of corticosteroid is sufficient to control the symptoms. This minimizes the amount of corticosteroid that is absorbed systemically, so reduces the occurrence of side effects which one would normally experience while on long-term oral corticosteroid use.

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afferent

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Towards CNS

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efferent

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away from CNS

motor division

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Somatic nervous system

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voluntary - skeletal muscle

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Autonomic nervous system

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involuntary- cardiac and smooth muscle, glands
sympathetic
parasympathetic

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Sympathetic

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"fight, flight, or fright"

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Parasympathetic

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"rest & digest"

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Acetylcholine (Ach)

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Chemical produced by the body that is used in the transmission of nerve impulses. It is destroyed by the enzyme cholinesterase

It is the primary neurotransmitter at the effector site for parasympathetic neurons.

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Adrenergic

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Refers to a drug stimulating a receptor for norepinephrine or epinephrine

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Antiadrenergic

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Refers to a drug blocking a receptor for norepinephrine or epinephrine

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Anticholinergic

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Refers to a drug blocking a receptor for acetylcholine

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Cholinergic

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Refers to a drug causing stimulation of a receptor for acetylcholine

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parasympatholytic

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= anitcholinergic

agent blocking or inhibiting the effects of the parasympathetic nervous system

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parasympathomimetic

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= cholinergic

agent causing stimulation of the parasympathetic nervous sytem

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sympatholytic

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=antiadrenergic

agent blocking or inhibiting the effect of the sympathetic nervous system

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sympathomimetic

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= adrenergic

Agent causing stimulation of the sympathetic nervous system

aka beta agonists, beta adrenergics - increase (catalyze) the production of cAMP

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Synapse

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a structure that permits a neuron to pass an electrical or chemical signal to another cell

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Effector site

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a nerve ending that carries impulses to a muscle, gland, or organ and activates muscle contraction or glandular secretion

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ganglion

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a group of nerve cells forming a nerve center, especially one located outside the brain or spinal cord.

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adrenal medulla

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adrenaline producing gland sitting atop the kidney.

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Norepenephrine (NE)

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the primary neurotransmitter in the sympathetic NS

Terminated by neurotransmitter reuptake intothe presynaptic neuron (uptake1) and by the enzymes COMT and MAO.

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nerve innervations

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the distribution of nerves across the body to particular areas

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uptake 1

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primary method NE is reabsorbed back into neuron

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catalyze

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increase the rate of something such as production

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cAMP

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(cyclic adenosine monophosphate) is a second messenger important in many biological processes.

cAMP is derived from adenosine triphosphate (ATP) and used for intracellular signal transduction in many different organisms, conveying the cAMP-dependent pathway

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transduction

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a mechanical / physical/etc stimulus is converted into an action potential

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phosphodiesterase

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any enzyme that breaks a bond. For us it is cAMP.

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phosphodiesterase inhibitors

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block the chemical breakdown of cAMP.

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Xanthines

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a group of drugs acting as phosphodiesterase inhibitors

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B1 receptor

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on the sympathetic side of the autonomic nervous system increases the rate and force of cardiac contraction when stimulated

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B2 receptor

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on the sympathetic side of the autonomic nervous system relaxes the smooth muscles in the bronchi when stimulated

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epinephrine

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beta neurotransmitter originating from the sympathetic nervous system in the form of NE norepenephrine or epinephrine

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Cholinesterase

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catalyses they lyses or destruction of ACh.

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muscarinic

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acetylcholine receptors on the parasympathetic NS side of the autonomic NS. To stimulate a parasympathomimetic a cholinergic would be utlized

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antimuscarinic

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agent used to block the action of ACh at the effector site in the parasympathetic side

AKA - Parasympatholytic

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cholinergic

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typically refers to acetycholine in the neurological sense.

cholinergic receptors respond to the neurotransmitter ACh.

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anticholinergic

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blocks the neurotransmitter ACh. Allows bronchodilation

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Adrenergic

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As a receptor, it responds to epinephrine or norepinephrine neurotransitters.

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adrenergic agonists

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(Based on naturally occurring epinephrine / Adrenaline in the body) stimulate/activate (agonist) the sympathetic NS receptors A, B1, B2

Specific to the sympathetic side of the NS

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Mast cells

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types of tissues that contains many granules rich in histamine and heparin. The cells degranulate during an allergy response releasing its contents into the blood stream

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mast cell stabilizers

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keep the mast cells from degranulating

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glucorticoids

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class of steroid hormones that bidn to the glucocorticoid receptor. GCs are part of the feedback mechanism in the immune system that turns immune activity (inflammation) down. Cortisol (or hydrocortisone) is the most important human glucocorticoid

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corticosteroids

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class of chemicals that includes steroid hormones naturally produced in the adrenal cortex. Corticosteroids are comprised if two major physiological groups: the glucocorticoids and the mineralcorticoids. However, the term corticosteroids is generally used to refer to glucocorticoids. Inhaled steroids include: Flunisolide Fluticasone Beclomethason Budesonide. The end desire is antimflammatory

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immunoglobulin E (IgE)

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class of antibody that manifests various allergic diseases, such as allergic asthma, allergic rhinitis, food allergies, and others

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antibody

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also known as an immunoglobulin (Ig)

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Leukotrienes

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a signaling fatty molecule that triggers contractions in the smooth muscles in the trachea; their overproduction is a major cause of inflammation in asthma and allergic rhinitis

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Lipoxygenase

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like a leukotriene similar response

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catecholamines

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Group of similar compounds having sympathomimetic action; they mimic the actions of epinephrine

in the human body, the most abundant catecholamines are epinephrine (adrenaline), norepiephrine (noradrenaline) and dopamine. Release of the hormones epinephrine and norepinephrine from the adrenalmedulla of the adrenal glads is part of the fight or flight response.

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chemical name

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the name of the drug in chemistry terminology complicated and rarely clinically used.

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Bronchorelaxation

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bronchodilation
Agonists at b2 adrenoceptors
Antagonists at M3 acetylcholine receptors

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Bronchoconstriction

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bronchospasm

Agonists at M3 acetylcholine receptors
Antagonists at b2 adrenoceptors

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neuromuscular junction

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myoneural junction.

The site where ACh conducts the nerve impulse at skeletal muscle sites

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neuroefffector site

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the terminal nerve site

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ACh is the neurotransmitter everywhere, except:

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at the sympathetic terminal nerve sites

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Adrenergic bronchodiator

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agent that stimulates sympathetic nervous fibers, which allow relaxation of sooth muscle in the airway.

Also known as sympathomimetic bronchodilator or B2 agonist

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a-receptor stimulation

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Causes vasoconstriction and vasopressor effect; in the upper airway (nasal passages), this can provide decongestion

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asthma paradox

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refers to the increasing incidence of asthma morbidity, despite advances in the understanding of asthma and availability of improved drugs to treat asthma.

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B1-receptor stimulation

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Causes increased myocardial conductivity and increased heart rate as well as increased contractile force.

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B2-receptor stimulation

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Causes relaxation of bronchial smooth muscle, with some inhibition of inflammatory mediator release and stimulation of mucociliary clearance.

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Bronchospasm

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Narrowing of the bronchial airways, caused by contraction of smooth muscle

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Cyclilc adenosine monophsophate (cAMP)

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Nucleotide produced by B2-receptor stimulation; it affects many cells, but causes relaxation of bronchial sooth mucle

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FEV

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Forced Expiratory volume

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Sympathomimetics

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stimulate production of cAMP

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Anticholinergics

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Block ACH at M1, M2, M3