Midterm 1 Flashcards
drug sources
Plants: morphine & codeine from poppy plant Digitalis is from the purple foxglove Quinine is from cinchona tree bark Paclitaxel is from the yew tree
Animals:
Insulin is obtained from pigs
Growth hormone is obtained from the pituitary glands
Bacteria:
Cephalosporins and ahminoglycosides
Chemical synthesis:
Most drugs today
Fentanyl
Minerals: vitamins
drug classification
Drugs that produce birth defects, such as thalidomide, are known asteratogens
Drugs that promote the growth of cancerous tumours are calledcarcinogens.
drug safety
Should be in therapeutic range
(TI) therapeutic index LD50/ED50 lethal dose, effective dose
what are drugs
chemical substance that produces a change In body function
Has specific chemical structure which means they have chemical and biological properties
Affect the functions of cells
side effects
More of a nuisance than they are harmful
Occur at minimal doses
adverse effects
Undesired effects that may be harmful
Reduction of stage or switching to an alternative drug often will avoid or minimize these consequences
Occur at high doses
toxic effects
Drug poisoning
Life threatening
Occur at very high doses
site of action
The location within the body where the drug exerts its therapeutic effect
drug forms
Aqueous Preparations - syrups, water and sugar combined with drug remove bitter taste of many drugs
Alcoholic preparations - elixirs are drugs dissolved in various concentrations of alcohol usually 5-20%
Solid and semisolid preparations - suppositories
Powders - drugs or drug extracts that are dried and ground into fine particles
Tablets - drug powders in convenient swallowing form and disintegrate in the stomach rapidly
Troches and lozenges - flattened tablets that dissolve in the mouth
Capsules - gelatin capsules used to administer drug powders or liquids, dissolve in the stomach
Delayed release products - tablets or capsules with a special coating so that various portions of the drug that will dissolve in certain rates, they usually contain 2-3 single dose units
Enteric coated products - drugs coated with an acid resistant substance that will dissolve in less acidic portions of the intestines, these drugs should be taken on an empty stomach with water 1 hour before meals or 2 hours after meals
Suppositories - drugs mixed with a substance that will melt at body temperature administered through the urethra, vagina or rectum
Ointments - soft, oily substances containing a drug that is applied to the skin or eye
Transdermal products - bandage/patch system provides continuous source of the drug over 24 hours
routes of administration
Oral - safest Sublingual Buccal Rectal Transdermal Subcutaneous Intramuscular Intravenous - fastest Intraarterial Intreathecal Inhalation -fastest Topical Vaginal
pharmacokinetics (dame)
study of the process of drug absorption, distribution, metabolism and excretion
lipid solubility
Most drugs are water soluble and only partially lipid soluble
ionization
Many water soluble drugs are weak acids or bases that can form charged particles (ionization)
Absorption is influenced by the degree of ionization
Most drugs exist in 2 forms ionized or unionized
drug formulation
Drugs must be in a solution to be absorbed
Lipid medications are absorbed faster then solids (smaller particles get absorbed faster)
drug distribution
Plasmas protein binding, blood flow and the presence of specific tissue barriers affect how much drug reaches a certain organ
plasma protein binding
Only unbound or free drug molecules can exert a pharmacological effect
When 2 drugs compete for one plasma protein binding site one may displace the other resulting in an increased free drug concentration which can lead to adverse effects
blood flow
Liver, kidneys, and brain have largest blood supply therefore are exposed to the largest amount of a drug
Fat has low blood supply but is high in lipids so lipid soluble drugs can enter fat easily
half life
amount of time it takes for the drug blood concentration to drop by half of its original level
bioavailability
the % of the drug absorbed into the blood stream
parasympathetic nerves
CN 3, oculomotor 7,9, and 10 vagus - supply the internal organs and glands of the head, thoracic cavity and upper portion of the abdominal cavity
S2-S4 - supply the lower portion of the abdominal cavity and the pelvic cavity
parasympathetic neurotransmitter
Acetylcholine (ACH) is the neurotransmitter released at the ganglion and at the post ganglionic nerve ending
Nerves that release (ACH) are known as cholinergic nerves
Cardiac and smooth muscle membrane sites where neurotransmitters act are known as cholinergic receptors
parasympathetic system roles
rest and digest
Theparasympatheticnervous system restores the body to a calm and composed state and prevents it from overworking
sympathetic nerves
T1-L3
Thoracic nerves supply the internal organs and glands of the head and the thoracic cavity and upper abdominal cavity
Lumbar nerves supply the lower portion of the abdominal cavity and the pelvic cavity
sympathetic neurotransmitters
(ACH) is released at the ganglion but norepinephrine (NE) is released at the post ganglionic nerve endings
Nerves that release (NE) are known as adrenergic nerves
Cardiac and smooth muscle membrane sites where neurotransmitters act are known as adrenergic receptors (2 types alpha and beta)
sympathetic nervous system is known as…
fight or flight system
peripheral (efferent) nerves
are branches of cranial and spinal nerves that travel to cardiac + smooth muscle of the internal organs
Composed of many neurons travelling together to the same destination
T/F
In ANS nerve 2 groups of neurons are linked together via synapses as the nerve travels from the spinal cord to the internal organ
T
pre ganglionic nerve fibre
neurons that emerge from the CNS to the ANS release neurotransmitter in post ACH released
post ganglionic nerve fibre
neurons that travel from the ganglion to the internal organ NE released
collection of synapses is called a…
ganglion
Norepinephrine
parent drug for the alpha drug class
must be administered by injection
short duration of action
contraction of smooth muscle
increases heart rate and blood pumping from the heart. It also increases blood pressure
Epinephrine
drug of choice fro immediate treatment for allergic reactions
subcutaneous administration is preferred
epi pen
also used in surgeries with local anesthetics to produce vasoconstriction
produced in adrenal medulla
not recommended for asthma because of cardiac stimulation
adrenergic receptors
alpha1 and alpha2
beta1 and beta2
some organs contain more then 1 receptor
alpha 1
smooth muscle
when stimulated by E/NE they contract
provides more blood to organs
alpha 2
located on adrenergic nerve endings
activate negative feedback
beta 1
smooth/cardiac muscle
when stimulated increase HR and force of contraction
beta 2
produce vasodilation, bronchodilation
increase blood flow to skeletal muscle and heart delivers more O2 to the lungs
alpha adverse effects
irritation to nasal sinuses and eyes
increased BP
cardiac arrhythmias
beta adverse effects
cardiac arrhythmias
restlessness
tremors
anxiety
albuterol
beta 2
bronchodilator
inhalant, tablet, syrup
dopamine
alpha
beta 1
circulatory shock
IV
epi table 6.4
alpha
beta
allergy
bronchodilator
SC, IM inhalant
chemical name
chemical or molecular structure
generic
nonproprietary
assigned by manufacture
trade name
proprietary
types of solutions
weight in weight
weight in volume
volume in volume
2 neurotransmitters in 2 ANS systems
acetylcholine
norepinephrine
2 types of adrenerdic receptors
beta (1/2) and alpha (1/2)
Cholinergic receptors
muscarinic and nicotinic
parasympathetic
muscarinic receptors
located on the cell membranes of visceral organs and glands
nicotinic receptors
nerves (NN) located on the cell membranes of visceral organs and glands on p/s systems
muscles (NM) located on cell membranes of skeletal muscle
adrenergic drug classes
sympathomimetics - stimulates the SNS
sympatholyics - antagonize the SNS
beta blockers are…
selective and non selective
atropine
tablet, parental injection
antidote for cholinesterase inhibitor poisoning, anticholinergic effects
opthalmic examinations
ipratropium
aerosol, inhaler
bronchodilator
anticholine drug adverse effects
dry mouth
visual disturbances
urinary retention
constipation
diancephalon includes…
the thalamus and the hypothalamus
the brainstem includes…
the midbrain, pons, medulla oblongata
limbic system
controls emotional behaviour/mental health
GABA
gamma aminobutyric acid
inhibitory neurotransmitter
accounts for 50% of the inhibitory activity of the brain and spinal cord
regulates the chloride channel
when gaba enters everything relaxes
Once gaba hits target cell it opens ion channel and allows more chloride to go into the cell
Chloride enters the cell and deactivates
when bound to GABAa receptor Cl channel opens
alcohol
most widely used non prescription sedative hypnotic and anti anxiety agent
alcohol pharmacology effects
depresses CNS
dilates vessels
stimulates secretion of saliva and gastric juice = increased appetite
gastritis
decreases renal absorption
lack of vitamins and amino acids
benzodiazepines
-class of drugs used to treat anxiety and sleep disorders
benzodiazepines MOA
-decrease excitibility/functional activity of certain areas of the brain and spinal cord (CNS)
-hyper polarization
-neuronal depression
increases inhibitory action of GABA which results in CNS depression
benzodiazepines adverse effects
- drowsiness
- confusion
- ataxia
- minor GI disturbances
- hangover effect
- insomnia
lorazepam
-anticonvulsant
-anti anxiety
-acts on the CNS to produce calming effect
-short duration (short acting)
-oral/iv/im
tonic clonic
-drug of choice for epilepticus
diazepam
- oral/iv/im
- anticonvulsant
- anti anxiety
- rapid onset
- long duration (long acting)
- alcohol withdrawl
- tonic clonic
long vs short acting benzos
- long acting half life of 20+ hours/from metabolites
- short acting half life of 5-20 hours/ metabolites dont contribute to the therapeutic affect
- metabolized by the liver
flumazenil
- antagonist of benzos
- IV
- reverse respiratory/CNS depression effects/OD
- may cause seizures
- reverse effects of midazolam in surgeries
midazolam
- preoperative sedation induction
- increase saliva and bronchospasm
- rapid onset
- drug of choice when parental is required
- IV/rectal
- potent short acting CNS depressant
- also used for induction of general anesthesia
- chosen because of its short half life and non active metabolites
pathways for pain
- start on nocireceptors
- travel through spinal cord through dorsal horn then to the appropriate vein to interpret intensity and quality of the pain
opioid clinical indications
- front line therapy for pain and pain associated procedures
- no increased risk of bleeding!
opioids
- bind to opioid receptors and mimicking the agonist affects
- inhibit nocireceptor signals from reaching the spinal cord
- contract bronchioles
- when bound to mu receptors Ca channels close
- K channels open
- dont give to people with head injuries
fentanyl
- chemically synthesized
- relieves acute and chronic pain
- preoperative sedation
- works on mu receptors
morphine
- standard opioid analgesic
- highly addictive
- wont work on pancreas
narloxone
- opioid antagonist
- do not produce opioid effects
- bind to receptors so other drugs cannot
- reverse mu effects
- life saving drug
cyclooxygenase
- family of enzymes required to make postglandins from arachidonic acid
- COX1 - always available in all cells so homeostasis is balanced
- COX2 - manufactured in activated microphages in response to injury or damaged local tissues
non opioid effects
- Do not depress cardiac function in therapeutic doses
- Hypotension
- May increase/decrease CNS
- GABA may be stimulated creating happy effect
- Other people may experience dysphoria
- Nausea/vomiting (not for some)
- Respiratory depression
- Moisis
- Increase smooth muscle tone
- Block release of ACH
- Increased pressure in the gall bladder
- Constrict bronchioles
- Decrease urine output
cholinergic receptor and nerve activity
- Anticholinergic drugs prevent ACH from acting on receptors
- 2 categories direct/indirect
- Direct acting drugs bind to receptors and produce effects similar to ACH and increase activity at the cholinergic sites
- Indirect acting drugs are known as anticholinesterases allow ACH to build up in receptor sites
action of non opioid anti inflammatory
- Ease symptoms associated with inflammation due to inhibition of prostaglandin synthesis
- 2 groups salicylates + NSAIDS and acetaminophen
- Produce analgesia and antipyresis by affecting the hypothalamus
- MOA involves blockade of prostaglandin stimulation of the CNS
- Vasodilators
- Inhibit COX
anti inflammatory adverse effects
- Vertigo
- Vomiting
- Confusion
- Headache
salicylates and NSAIDS
- Aspirin (drug of choice for fevers) and salicylic acid (plant based)
- Oldest and most frequently used
- Improve minor aches and pains
- Aspirin shouldn’t be taken while pregnant
- Children and teenagers recovering from chicken pox/flu shot not use these products due to the risk of
- Reyes syndrome (swelling in liver and brain)
acetaminophen
- Aspirin substitute
- No proven anti inflammatory activity
- Drug of choice for fever and cold relief for children
- Doesn’t irritate the stomach lining like aspirin
- Tylenol
- Can contribute to liver failure
acetaminophen adverse effects
- Nausea/vomiting
- Flu like symptoms
- Liver toxicity
non-steroidal inflammatory
- Used for short periods (7 days)
- Advil
- Tylenol
- Asa
epi vs norepi in regards to smooth muscle
- epi relaxes smooth muscle
- norepi doesn’t
beta blockers suffix
LOL
phenytoin
dilantin works on sodium channels
tonic clonic =
grand mal
alcohol provides a ? effect to the skin
cooling
reticular fibres
- network of nerve fibres that travel through the brain and spinal cord
- Composed of excitatory fibres
- Composed of inhibitory fibres
frontal lobe
-muscle movement (stroke here will have hard time talking, moving)
parietal lobe
- touch
- vibrations
temporal lobe
-language
occipital
- communication
- coordination
- vision
cerebellum
- body movement
- posture
hypothalamus
- body temp
- energy maintenance
1 teaspoon =
5 ml
1 table spoon =
15ml or 1/2 oz
how many drops is a teaspoon
60
