Midterm 2 Part 2 Flashcards

1
Q

Where are weak acids better absorbed?

A

stomach

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2
Q

Where are weak bases better absorbed?

A

intestine

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3
Q

bioassay

A

provides information on the pharmacological activity of new or chemically-undefined substances

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4
Q

pharmacodynamics

A

What the drug does to the body
Quantitative relationship between concentration and receptor interaction AND specific cellular response

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5
Q

Steeper quantal dose response curve means

A

lower variation in the population

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5
Q

Less steep, slow-rising quantal dose response curve means

A

higher variation in the population

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6
Q

Minimal effective dose, MED

A

Lowest dose that will produce the desired therapeutic respond

Makes up the lower part of the therapeutic window

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7
Q

Maximum tolerated dose (MTD)

A

highest dose that can be administered w/o adverse/toxic effects

Makes up the higher part of the therapeutic window

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8
Q

ED50

A

Effective dose in 50% of the concentration

Makes the lower part of the therapeutic index

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9
Q

TD50

A

toxic effect in 50% of the population at this dose

Makes up the upper part of the therapeutic index

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10
Q

Potency

A

A comparative expression of drug activity.
Does not indicate efficacy. Just because one drug is more potent, doesn’t mean it is more effective

Potency increases as EC50 decreases

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11
Q

What receptor is LSD an agonist for?

A

serotonin receptor. It is less potent than serotonin however.

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12
Q

Non-competitive antagonists

A

Bind to allosteric site rather than orthostatic site. Form a strong bond and thus slowly or does not dissociate from receptor –insurmountable because you can’t add more agonist to displace the antagonist. Emax decreases

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13
Q

Psychoactive drug

A

Drug that affects the CNS and alters behaviour including mood and cognition
Can be therapeutic or recreational

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14
Q

Tolerance

A

When repeated exposure to drugs decreases effectiveness of the drug. Lower response to a given dose of drug.
Need higher dose to get the same ‘desired’ effect

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15
Q

METABOLIC tolerance

A

body gets more efficient at elimination of the drug

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16
Q

cellular tolerance

A

target tissue has decrease sensitivity. The number of receptors is reduced or else they just become less sensitive

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17
Q

How are some ways the body will try to maintain homeostasis when on drugs?

A

If taking an agonist - body might try to reduce the receptors to reduce the response
If taking on antagonist - body might try to increase the number of receptors to increase the response

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18
Q

Learned tolerance

A

Adapt behaviour based off experience to compensate for the effects of the drug. Consciously or unconsciously you have learned how you respond to the drug.
Lowers the response

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19
Q

Cross tolerance

A

Tolerance of one drug can be transferred over to another drug within the same family. Therefore, you can exhibit tolerance for a drug that you have never taken before.

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20
Q

Drug sensitization

A

Intermittent exposure to a drug can lead to enhanced responses to subsequent exposure to the same dose.
Can last a long time and occur after a single use.

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21
Q

Amphetamines

A

Enhance the release of dopamine AND block re-uptake transporters of NE, 5-HT, and dopamine. 1

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22
Q

Caffeine

A

Is an antagonist that binds to caffeine receptors and prevents a response from occurring.
Caffeine tolerance - neurons synthesize more adenosine receptors - makes it so that more caffeine is required to block the additional receptors.
- SO when you stop drinking coffee and have many receptors - increased sensitivity to adenosine - sleepy

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23
Q

Nicotine

A

Binds and activates the nicotinic ACh receptor (Na+ flows in)
At low initial doses - acts as a stimulant
At high initial does - acts as a relaxant

Leads to release of dopamine
Rapid tolerance

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24
Q

Acetylcholinesterase inhibitors

A

Used for treatment of Alzheimers and dementia

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25
Q

Benzodiazepines

A

AFFECT GABA receptor. They bind to the receptor and promote the influx of chorine ions into the cell. Therefore - they reduce the responsiveness of the cell.

Used for anxiety, sleep, epilepsy
They decrease sleep problems by decreasing neuronal activity

26
Q

GABA receptor agonists

A

Benzodiazapines, alcohol, GABA

27
Q

Alcohol

A

GABA receptor agonist. Promotes the influx of chloride ions
Excessive usage can lead to nerve damage, cortical loss, and decreased neurogenesis

28
Q

What happens if you have a poor diet and drink lots of alcohol?

A

Thiamine deficiency - Korsakoff’s Syndrome

29
Q

What is the main excitatory neuron in the forebrain and cerebellum?

A

Glutamate. Involved in learning and memory

30
Q

Phencycladine

A

PCP; angel dust
Hallucinogenic, cognitive impairment
Act by blocking NMDA receptors (these receptors are essential for synaptic plasticity - learning/memory)

Drug affecting glutamate

31
Q

Ketamine

A

Dissociative anaesthetic. Low IV doses showing benefits for depression
Act by blocking NMDA receptors (these receptors are essential for synaptic plasticity -learning/memory)q

32
Q

Monoamine oxidase inhibitors (MAOI)

A

Inhibit the breakdown of 5HT in the presynaptic terminal so that more serotonin is available for release

33
Q

5-HT receptor agonists

A

LSD, mescaline, ecstasy - all hallucinogenic

34
Q

therapeutic lag

A

When a drug takes some time to make a noticeable difference in the body. Characteristic of some serotonin anti-depressants

35
Q

SSRIs and tricyclics

A

Block transporter protein for the re-uptake of serotonin

36
Q

LSD

A

partial agonist for serotonin receptor
increase glutamate transmission in the frontal cortex
Has rapid tolerance (down regulation of the serotonin receptor)
Not considered toxic or addictive

37
Q

Schizophrenia

A

Associated with excessive MESOLIMBIC dopaminergic activity

Antipsychotics decrease dopaminergic related activity particularly in the frontal lobe

Best treated with ATYPICAL NEUROLEPTICS

38
Q

What meds are the best to treat Schizophrenia and why?

A

Atypical neuroleptics because these don’t cause as many movement problems (from decreasing dopamine too much - Parkinson’s symptom)

39
Q

1st generation neurolyptics

A

anti-pschotics used originally to treat schizophrenia (decrease dopamine)

They act as D2 antagonists (they prevent dopamine release from the presynaptic terminal- cause movement problems - with Parkinson’s - don’t get enough dopamine production and get movement problems.

40
Q

ADHD

A

Used to treat with dopamine agonists
Drug treatment involves preventing the reuptake of dopamine and or NE from the synapse - enhance activity at the synapse - better control attention and behaviour

41
Q

How do cocaine and amphetamines act?

A

THey work in a similar fashion to ADHD treatment drugs –> block uptake of Dopamine and NE - increase activity - agonist

41
Q

How do cocaine and amphetamines act?

A

THey work in a similar fashion to ADHD treatment drugs –> block uptake of Dopamine and NE - increase activity - agonist

42
Q

Parkinson’s disease

A

Disease associated with loss of neurons producing dopamine in the mesolimbic area. not enough dopamine production

Treatment with L-Dopa is good but need to combine treatment with benserazide to prevent adverse effects in the body as there are dopaminergic neurons outside of the brain.

43
Q

Benserazide

A

Inhibits DOPA decarboxylase. This is important when treating Parkinson’s disease to lower adverse effects in the body.
Given in combination with L-Dopa
Cannot cross the BBB
Prevents the formation of excessive dopamine in the body but still allowing formation of dopamine in the brain as it does not cross the BBB

44
Q

Treatment for Parkinsons

A

L-Dopa and Benserazide

45
Q

Opiates

A

Agonists to the opiate receptor (GPCR)
Used for pain relief, medicinal and recreational use
Can be converted into morphine, codeine, heroin

Endogenous opioid receptor ligands: enkephalins, endorphins (can activate AC or an ion channel)

Major drug abuse substance
Can get tolerance or sensitiziation
overdose risk

Excessive stimulation

46
Q

Endogenous opioid receptor agonist ligands

A

Enkephalins, endorphins

47
Q

What is an antagonist for opiates?

A

naloxone

48
Q

Cannabis

A

Contains 84 active incredients including THC and CBD
Activate endocannabinoid receptors

49
Q

What is the primary component of cannabis that causes psychoactive effects?

A

THC
too much THC can lead to paranoia and hallucinations

50
Q

Medicinal uses for cannabinoids?

A

Glaucoma, chronic pain, decreasing nausea

51
Q

Cannabidiol

A

CBD - pure. CLinical use -Don’t get hallucinations like with THC overusage
May help with epilepsy and other things

52
Q

Substance abuse

A

Drug use when a person relies on a drug and its use becomes a major component in their life

53
Q

Addiction

A

Substance DEPENDANCE
Escalating, compulsive, relapsing
Disproportionate amount of time seeking, preparing and consuming the drug
Interferes with everyday life
Even if you want to stop, its very difficult to actually stop
Want the drug, even if you don’t like the drug

54
Q

Escalation of drug consumption

A

increasing in dose and frequency of taking the drug.

MORE THAN SIMPLY TOLERANCE

transformation of drug abuser to drug addict

55
Q

How does a drug addiction form?

A

Psychomotor activation - give an energized feeling
Activation of the dopaminergic system either directly (cocaine) or indirectly (ventral tegmentum - nucleus accumbens)

Drugs that block this reward pathway can help with addiction

56
Q

Hedonia hypothesis

A

Addictions form due to pleasure?
ie sex, food, sports, excitement
- endorphins produced that give a high
After the initial pleasures wear off - user is still wanting (craving) the drug

57
Q

allomone

A

hormone released to attract other species

58
Q

Protein hormones

A

String of amino acids. Water soluble
Most bind to R on the cell membrane - often kinase-linked - activate second messenger pathways

59
Q

Amine hormones

A

Based off of a single amino acid
Tyrosine or tryptophan w/modified groups
WAtersoluble

Most bind to R on the cell membrane - often kinase-linked - activate second messenger pathways

60
Q

Base AA for amino hormones?

A

Tyr Trp

61
Q

Steroid hormones

A

based on a cholesterol molecule
LIPID soluble
Cholesterol is essential to make these hormones