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Pharm 100 > Midterm prep > Flashcards

Midterm prep Flashcards

1
Q

the 5 key steps in the drug development process

A

basic research and drug discovery

preclinical trials

clinical trials

health canada review and manufacturing

post market surveillance and phase IV clinical trials

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2
Q

basic research involves

A

identification of the target

studying of the target

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3
Q

preclinical studies involve

A

pharmacology studies - mechanism of action

toxicology studies

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4
Q

compare phase 1, 2 and 3 trials

A
  • Phase 1 (proof of safety)
    ○ Tests the absorption, distribution, elimination and adverse effects of the drug - the tolerability
    ○ Conducted in a limited number of healthy volunteers, do not assess the efficacy of the drug
  • Phase 2 (methodology)
    ○ Look to determine whether the drug is effective in treating the condition for which it is recommended
    ○ Safety of drug
    ○ Patients have the disease–

Phase 3 (investigation)
○ Randomized control trials
○ Used for the licencing and marketing of the drug
○ How safe and effective compared to placebo or current treatment

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5
Q

what composes drug action

A

drug targets, therapeutic range, drug response and efficacy/potency

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6
Q

what is threshold of effect

A

Once this threshold is reached, small increase in dose will result in a large increase in response (therapeutic doses)

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7
Q

efficacy vs potency

A
  • Efficacy
    ○ The maximum pharmacological response that can be produced by a specific drug in that biological system
    • Potency
      ○ The dose of a drug that is required to produce a response of a certain magnitude - usually 50% of the maximal response
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8
Q

what are the 3 ways to administer a drug

A

topical (inhalation or the skin)

enteral (GI tract)

parenteral (bypasses GI tract)

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9
Q

adverse effects of drugs

A

-extension of the therapeutic effect (overdose)
-unrelated to main drug action (Nausea)
-allergic reaction
-withdrawal/addiction
-teratogenesis
-adveerse biotransfomation reaction

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10
Q

list some drug-food interactions

A

tyramine (found in well mature cheeses)
- MAO interaction with antidepressants and raises blood pressure

grapefruit
-alter absorption, inhibit enzymes that inactivate drugs

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11
Q

what part of the brain is often misuses with drugs/associated with addiction due to its dopaminergic reward centers

A

limbic system - hypothalamus

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12
Q

how do drugs cross membranes

A
  • Passive diffusion
    ○ Most prevalent
    • Active transport
      ○ Channel mediated
    • Filtration via pores
      Only for very small drugs that are water soluble
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13
Q

what is biotransformation

A

the conversion of a drug to a different chemical compound in order to eliminate it

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14
Q

ways drugs can be excreted

A

§ Majority from kidney
§ GI tract
§ Volatile or gaseous can be excreted by the lungs
§ Saliva and sweat

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15
Q

what is bioavailability

A
  • The fraction of an administered dose that reaches systemic circulation in an active form
    • In percent
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16
Q

what are the catecholamines

A

dopamine - addiction (motivation and reward)
norepinephrine - excitatory

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17
Q

do stimulants increase or decrease serotonin at the synapse

A

increase

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18
Q

what response do cholinergic (acetylcholine) receptors do

A

excitatory

there is nicotinic and muscarinic receptors

19
Q

general criteria for SUD

A

risky use

social impairments

impaired control

withdrawal

tolerance

19
Q

what is addiction

A
  • A state in which stopping or abruptly reducing the dose of a given drug produces non physical symptoms
20
Q

characteristics of addictive drugs

A

increase dopamine

induce novelty

reduce anxiety

20
Q

name some stimulants

A

cocaine
amphetamines
nicotine
caffeine

21
Q

describe drug withdrawal symptoms

A
  • Stimulants
    ○ Sleepiness, muscle pain, anxiety, tremors, low mood, suicidal ideations and cardiovascular problems in some cases
    • Opioids
      ○ Sweating, muscle aches, agitation, diarrhea, abdominal cramping, vomiting
22
Q

describe drug tolerance

A

Repeated administration of a given dose has less and less pharmacological effect OR drug must be increased to get the same effect

23
Q

what increases potential for misuse

A
  • Nature of the drug
    ○ Drugs are natural reinforcers
    • Route of administration
      ○ Rapid absorption and rapid effects
    • Amount/frequency of use
      ○ Greater dose and frequency, the greater potential for misuse
    • Availability
      ○ Alcohol
    • Inherent harmfulness
      ○ Potential for the drug to cause harm
24
Q

how do amphetamines work in the brain

A

increase free dopamine/norepinephrine

block VMAT so dopamine cant be packaged for release when the next nerve impulse arrives - forcing it back through the dopamine transporter into the synaptic cleft, increasing activity

25
Q

CNS effects of amphetamines

A
  1. Decreased threshold for transmitting sensory input to the cerebral cortex, leading to CNS excitation
    1. A feeling of euphoria and reward
    2. Temperature regulation and feeding centre modifications leading to appetite suppression
    3. An increase in aggressive behaviour and mood swings
26
Q

how does cocaine work in the brain

A

inhibits the reuptake of dopamine and serotonin into the presynaptic neuron

increases amount in synaptic cleft and therefore activity of the postsynaptic neuron

27
Q

how is nicotine excreted

A

urine

28
Q

amphetamines are used in sport for

A

endurance and speed, they are powerful psychomotor stimulants

mask pain/fatigue

29
Q

what is the goal of blood doping

A

to improve oxygen circulation

30
Q

anabolic steroids are used in sports for

A

increasing muscle mass and strength

31
Q

what do CNS depressants treat

A

anxiety disorders, sedation, hypnosis (sleep), general anesthesia

32
Q

how do CNS depressants work

A

decreasing glutamate induced nerve firing

increase inhibitory signals from GABA, GABA works with the chloride channel

33
Q

benzodiazepines increase

A

the frequency of opening the chloride channel

34
Q

what is the antidote for benzoiazepines

A

flumazenil

35
Q

barbituates increase

A

the duration the chloride channel is open

36
Q

buspirone doesnt act on GABA, it acts on

A

the serotonin receptor

advantageous in that it isnt additive with other CNS depressants

37
Q

what are the steps of alcohol metabolism

A

ethanol-> acetaldyhyde by ADH -> Acetate by ADLH -> CO2 and water

38
Q

what is the rate limiting step in alcohol metabolism

A

alcohol dehydrogenase

39
Q

mechanism of action of alcohol

A
  • Binds to the chloride ion channel and augments GABA mediated neuronal inhibition
    • Reinforcement of the drug may be explained by the interaction with the chloride ion channels of dopaminergic neurons in the reward centers of the brain
40
Q

drugs used to treat alcohol use disorder

A

naltrexone: an opioid antagonist, diminishes cravings by blocking reward pathways

benzos, manage withdrawal symptoms

41
Q

the classes of opioids

A

endogenous

natural (morphine/codeine)

semi synthetic (heroin)

synthetic (fentanyl)

42
Q

opioid receptors

A
  • MU
    ○ Brain and spinal cord
    ○ Mediate analgesia and responsible for morphine mediated depression of respiration in the brain stem
    ○ Misuse of opioids
    • KAPPA
      ○ Analgesia
      ○ Dysphoria
      § State of dissatisfaction or unease
      ○ Miosis
      § Pinpoint pupils
    • DELTA
      ○ Analgesia in spinal cord and brain
      Emotional response to opioids

Pharm 100 (2 decks)

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