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PSYC 211 > L07 > Flashcards

L07 Flashcards

1
Q

What is an abnormal condition of the mind that results in difficulties determining what is real and what is not real and that affects about 1% of the population?

A

Psychosis

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2
Q

What are the symptoms of psychosis?

A

Symptoms may include delusions, hallucinations, incoherent speech, and behavior that is inappropriate for the situation.

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3
Q

What are antipsychotics?

A

A class of drugs used to treat psychosis.
They are mostly dirty drugs, which means they bind to more than type of receptor, but the one action they all have in common is they directly block the dopamine D2 receptor, which is an inhibitory metabotropic receptor expressed by neurons all over the brain.

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4
Q

While some drugs are used to treat mental illness, others are used _____.

A

recreationally

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5
Q

What do drugs that cause hallucinations regularly activate?

A

Serotonin 2A receptors, which are inhibitory metabotropic receptors expressed by neurons all over the brain.

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6
Q

Do all direct serotonin 2A receptor agonists cause hallucinations?

A

No. Some 5HT-2A receptor agonists cause massive hallucinations while others do nothing of the sort.

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7
Q

What are the 4 drugs that directly activate serotonin 2A receptors?

A

Mescaline, psilocybin, LSD (hallucinogens)
Lisuride (not a hallucinogen)

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8
Q

What happens when a drug (non hallucinogenic) that activates serotonin 2A receptors bind?

A

When these agonists bind and activate this metabotropic receptor, they launch an intracellular signaling cascade that starts with the g protein ‘Gq/11’. Serotonin normally activates this receptor the same way.

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9
Q

What happens when a hallucinogenic drug that activates serotonin 2A receptors bind?

A

It turns out that hallucinogenic drugs activate the serotonin 2A receptor in a slightly different way, which stimulates an additional g protein known as ‘Gi/o’ (not just Gq/11). It is the 5HT2A receptor-induced activation of Gi/o proteins that causes hallucinations.

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10
Q

What is biased agonism?

A

When a metabotropic receptor ligand causes the receptor to preferentially activate one type of intracellular g protein, whereas another ligand at the same receptor might preferentially activate a different g protein.

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11
Q

What are direct agonists/antagonists?

A

Drugs that affect postsynaptic receptor activity by directly binding to postsynaptic receptors.

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12
Q

What are indirect agonists/antagonists?

A

Drugs that affect postsynaptic receptor activity in an indirect manner; the proteins they bind to are not postsynaptic receptors.

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13
Q

What is a receptor agonist?

A

A drug that directly or indirectly increases the activity of postsynaptic receptor proteins

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14
Q

What is a receptor antagonist?

A

A drug that directly or indirectly decreases the activity of postsynaptic receptor proteins.

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15
Q

How can drugs be categorized?

A
  1. According to their behavioral effects (ex: upper, downer, stimulant)
  2. According to their physiological effects (ex: action potential blocker)
  3. According to their actions on specific proteins (ex: serotonin reuptake blocker)
  4. According to their effects on postsynaptic receptor activity
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16
Q

Direct agonists can be classified as _____ or _____.

A

competitive, non-competitive

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17
Q

What are direct competitive agonists and what do they do?

A

A competitive agonist activates the receptor by binding where the neurotransmitter normally binds.
They can be full agonists or partial agonists.

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18
Q

What are direct competitive antagonists and what do they do?

A

A competitive antagonist attaches to the same binding where the neurotransmitter normally binds, but it doesn’t activate the receptor. Competitive antagonists are full antagonists.

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19
Q

What will the competition for a binding site between an endogenous neurotransmitter and an exogenous drug depend on?

A

Their relative concentrations and their affinity for the binding site.

20
Q

What does affinity refer to?

A

Affinity refers to the probability and tightness of ligand-receptor binding.

21
Q

What is non-competitive binding?

A

When a drug binds to a receptor at a site that does not interfere with the binding site of the principal ligand. It is possible for a neurotransmitter to bind on one site of a receptor while a drug binds on another.

22
Q

What does a non-competitive agonist do?

A

It fully or partially activates the receptor.

23
Q

What does a non-competitive antagonist do?

A

It fully blocks receptor activation. It doesn’t compete for the neurotransmitter binding site. It “wins” without competing by binding to an alternative site.

24
Q

What are allosteric modulators?

A

Non-competitive drugs that only influence receptor activity when the neurotransmitter is also bound to the receptor.

25
Q

What do positive allosteric modulators do?

A

They amplify the effect of the primary ligand.

26
Q

What do negative allosteric modulators do?

A

They reduce the effect of the primary ligand.

27
Q

What is Parkinson’s disease caused by?

A

The degeneration (death) of dopamine neurons in the midbrain.

28
Q

What amino acid is often used as a drug to treat Parkinson’s disease?

A

L-Dopa. It increases dopamine production in the brain and thus acts as an indirect dopamine receptor agonist.

29
Q

What are examples of drugs that block the reuptake of catecholamine neurotransmitters?

A

Methlyphenidate and cocaine.
They block the dopamine and norepinephrine reuptake transporters.

30
Q

What are examples of drugs that reverse catecholamine transporters?

A

Adderall and crystal meth.
They cause dopamine and norepinephrine molecules to flow directly out of the presynaptic terminal (non-vesicular release).
[Ecstasy (MDMA) does a similar thing to all the monoamine transporters (i.e. causes them to run backwards).]

31
Q

What is a dose response curve?

A

A graph of the magnitude of an effect of a drug as a function of the amount that is administered. It is obtained by giving subjects various doses of drug (typically according to weight).
-Higher doses cause larger effects until the point of maximum effect

32
Q

How do we call the difference between the 2 curves in a dose response curve?

A

The margin of safety or the therapeutic index, which represent the ratio between the dose that produces a toxic effect in 50 percent of animals, and the dose that produces the desired effect in 50 percent of animals.

33
Q

What are pharmacokinetics?

A

The process by which drugs are absorbed, distributed within the body, broken down, and excreted.

34
Q

What does the route of administration affect?

A

It affects where the drug goes, in what quantity, and for how long. There are many ways to get drugs inside the body and brain.

35
Q

What are the 3 key considerations when choosing a route of administration?

A
  1. Does the drug naturally cross the blood-brain barrier?
  2. Is it better to have a high concentration of drug for a short time or a low concentration of drug for a long time?
  3. Where in the body are there enzymes that break down the drug? In the stomach, blood, liver, brain?
36
Q

What is an intraperitoneal (i.p.) injection?

A

An injection into the abdominal wall (peritoneal cavity).

37
Q

What is an intravenous (i.v) injection?

A

An injection into the veins

38
Q

What is an intracerebral administration?

A

An injection directly into the brain

39
Q

What is an intracerebroventricular injection?

A

An injection into a cerebral ventricle

40
Q

What is an intrathecal (epidural) injection?

A

An injection into the cerebrospinal fluid of the spinal cord

41
Q

What is tolerance?

A

When an effect of the drug diminishes because of repeated administration. It is the body’s attempt to compensate for the effects of the drug.
Ex: A regular heroin user must take larger and larger amounts of the drug to keep feeling the same effect. Having developed tolerance to heroin, the user will suffer withdrawal symptoms which are opposite effects of the drug (i.e., euphoria vs dysphoria).
Ex: Barbiturates have sedative and depressive effects. The sedative effect shows tolerance, but the depressive effect does not. Thus, if larger doses of barbiturates are taken to achieve a sedative effect, you run the risk of taking a dangerously high dose of the drug and have depression.

42
Q

What is sensitization?

A

Sensitization occurs when a drug becomes more and more effective through repeated use.

43
Q

What is a placebo?

A

An inert substance that has no direct physiological effect. It is given to subjects to control the effects of mere administration of a drug.

44
Q

Does heroin cross the blood-brain barrier?

A

Yes. It crosses the blood-brain barrier quickly
because it is very lipid (fat) soluble.

45
Q

Does morphine cross the blood-brain barrier?

A

Yes, but it crosses the blood-brain barrier a bit slower than heroin because it is less lipid soluble.

46
Q

Does Imodium (anti-diarrheal) cross the blood-brain barrier?

A

No

47
Q

What are examples of very strong opiates?

A

Heroin, morphine, and imodium

PSYC 211 (8 decks)

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